Recent Publications

2020

2019

2018

2017

Syeda, S. S.; Rice, D.; Hook, D. J.; Heckert, L. L.; Georg, G. I. Synthesis of Arylazide- and Diazirine-Containing CrAsH-EDT2 Photoaffinity Probes. Arch. Pharm. (Weinheim). 2016, 349, 233-241. DOI: 10.1002/ardp.201500440

Shetty, J.; Sinville, R.; Shumilin, I. A.; Minor, W.; Zhang, J.; Hawkinson, J. E.; Georg, G. I.; Flickender, C. J.; Herr, J. C. Recombinant production of enzymatically active male contraceptive drug target hTSSK2 - Localization of the TSKS domain phosphorylated by TSSK2. Protein Expression Purif. 2016, 121, 88-96. DOI: 10.1016/j.pep.2016.01.009

Syeda, S. S.; Carlson, E. J.; Miller, M. R.; Francis, R.; Clapham, D. E.; Lishko, P. V.; Hawkinson, J. E.; Hook, D.; Georg, G. I. The Fungal Sexual Hormone Sirenin Activates the Human CatSper Channel Complex. ACS Chem. Biol. 2016, 11, 452-459. DOI: 10.1021/acschembio.5b00748

Zhang, Y.; Matsuyama, H.; Shiratsuchi, T.; Tian, D.; Hook, D. J.; Walters, M. A.; Georg, G. I.; Hawkinson, J. E.; Hamazaki, T.; Terada N. Human Adenine Nucleotide Translocase (ANT) Modulators Identified by High-Throughput Screening of Transgenic Yeast. J. Biomol. Screen. 2016, 21, 381-390. DOI: 10.1177/1087057115624637

2015

Li, W.; Georg, G.I.; Schneider, C.M. Synthesis of strained 1,3-diene macrocycles via copper-mediated Castro-Stephens coupling/alkyne reduction tandem reactions. Org. Lett. 2015, 17, 3902-3905. DOI: 10.1021/acs.orglett.5b01892

Siegel, R.A.; Kapoor, M.; Cheryala, N.; Georg, G.I.; Cloyd, J.C. Water-soluble benzodiazepine prodrug/enzyme combinations for intranasal rescue therapies. Epilepsy & Behavior 2015, 49, 347-350. DOI: 10.1016/j.yebeh.2015.05.004

Kirtane, A.R.; Wong, H.L.; Guru, B.R.; Lis, L.G.; Georg, G.I.; Gurvich, V.J.; Panyam, J. Reformulating tylocrebrine in epidermal growth factor receptor targeted polymeric nanoparticles improves its therapeutic index. Mol. Pharm. 2015, 12, 2912-2923. DOI: 10.1021/acs.molpharmaceut.5b00173 *ACS Editors Choice: Selected for Open Access*

Gu, X.; Georg, G. I. Regioselective C5-Alkylation and C5-Methylcarbamate Formation of 2,3-dihydro-4-pyridones and C3-Alkylation and C3-Methylcarbamate Formation of 4-(Pyrrolidin-1-yl)furan-2(5H)-one. Tet. Lett. 2015, 56, 5874-5877. DOI:10.1016/j.tetlet.2015.09.004

Holth, T. A. D.; Hutt, O.; Georg, G. I. Beckmann Rearrangements and Fragmentations in Organic Synthesis. In Molecular Rearrangements in Organic Synthesis. Editor Christian Rojas, Wiley: Book Chapter, 2015. ISBN: 978-1-118-34796-6.

Li, W.; Georg, G.I. A concise formal total synthesis of lactidomycin. Chem. Comm. 2015, 51, 8634-8636. DOI: 10.1039/C5CC02571K

Syeda, S.S.; Jakkaraj, S.; Georg, G.I. Scalable syntheses of the BET bromodomain inhibitor JQ1. Tet. Lett. 2015, 56, 3454-3457. DOI: 10.1016/j/tetlet.2015.02.062

Olsen, S.H.; Ingles, D.J.; Zhu, J-Y.; Martin, M.P.; Betzi, S.; Georg, G.I.; Tash, J.S.; Schonbrunn, E. Stability of the human Hsp90-p50Cdc37 chaperone complex against nucleotides and Hsp90 inhibitors, and the influence of phosphorylation by casein kinase 2. Molecules. 2015, 20, 1643-1660. DOI:10.3390/molecules20011643

Patil, S.; Lis, L. G.; Schumacher, R. J.; Norris, B. J.; Morgan, M. L.; Cuellar, R. A. D.; Blazar, B. R.; Suryanarayanan, R.; Gurvich, V. J.; Georg, G. I. Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficay in Human Colon adenocarcinoma and Ovarian Cancer. J. Med. Chem. 2015, 58, 9334-9344. DOI: 10.1021/acs.jmedchem.5b01329 *ACS Editors Choice: Selected for Open Access*

2013

Martin, M.P.; Olesen, S.H.; Georg, G.I.; Schonbrunn, E. Cyclin-dependent kinase inhibitor dinaciclib interacts with the acetyl-lysine recognition site of bromodomains. ACS Chem. Biol. 2013, 8, 2360-2365. DOI: 10.1021/cb4003283

Yu, Y-Y.; Georg, G.I. Dehydrogenative alkenylation of uracils via palladium-catalyzed regioselective C-H activation. Chem. Comm. 2013, 49, 3694-3696. DOI: 10.1039/C3CC41130C

Schonbrunn, E.; Betzi, S.; Alam, R.; Martin, M.P.; Becker, A.; Han, H.; Francis, R.; Chakrasali, R.; Jakkaraj, S.; Kazi, A.; Sebti, S.M.; Cubitt, C.L.; Gebhard, A.W.; Hazlehurst, L.A.; Tash, J.S.; Georg, G.I. Development of highly potent and selective diaminothiazole inhibitors of cyclin-dependent kinases. J. Med. Chem. 2013, 56, 3768-3782. DOI: 10.1021/jm301234k

Gu, X.; Georg, G.I. Lithium perchlorate-, acetic anhydride-, and triphenylphosphine-assisted multicomponent syntheses of 4-unsubstituted 2,5-dioxooctahydroquinoline-3-carboxylates and 3-carbonitriles. Tetrahedron. 2013, 69, 9406-9416. DOI: 10.106/j.tet.2013.08.081

Yu, Y-Y.; Bi, L.; Georg, G.I. Palladium-catalyzed direct C-H arylation of cyclic enaminones with aryl iodides. J. Org. Chem. 2013, 78, 6163-6169. DOI: 10.1021/jo400830t

Chung, S.S.W.; Cuellar, R.A.D.; Wang, X.; Reczek, P.R.; Georg, G.I.; Wolgemuth, D.J. Pharmacological activity of retinoic acid receptor alpha-selective antagonists in vitro and in vivo. ACS Med. Chem. Lett. 2013, 4, 446-450. DOI: 10.1021/ml300365k

Hutt, O.E.; Doan, T.L. Georg, G.I. Synthesis of skeletally diverse and stereochemically complex library templates derived from isosteviol and steviol. Org. Lett. 2013, 15, 1602-1605. DOI: 10.1021/ol400385w 

2012

Chugh, R.; Sangwan, V.; Patil, S.P.; Dudeja, V.; Dawra, R.K.; Banerjee, S.; Schumacher, R.J.; Blazar, B.R.; Georg, G.I.; Vickers, S.M.; Saluja, A.K. A preclinical evaluation of Minnelide as a therapeutic agent against pancreatic cancer. Sci. Transl. Med. 2012, 4, 156ra139. DOI: 10.1126/scitranslmed.3004334  *Highlighted by Science News November 18, 2012*

Kim, Y.W.; Niphakis, M.J.; Georg, G.I. Copper-assisted palladium(II)-catalyzed direct arylation of cyclic enaminones with arylboronic acids. J. Org. Chem. 2012, 77, 9496-9503. DOI: 10.1021/jo301531k *Featured Article in The Journal of Organic Chemistry* *Featured in KemKat’s Synthetic Abstracts*

Lee, J.C.; Francis, S.; Dutta, D.; Gupta, V.; Yang, Y.; Zhu, J-Y.; Tash, J.; Schonbrunn, E.; Georg, G.I. Synthesis and evaluation of eight- and four-membered imino-sugar analogs as inhibitors of testicular ceramide-specific glucosyltransferase, testicular beta-glucosidase 2, and other glycosidases. J. Org. Chem. 2012, 77, 3082-3098. DOI: 10.1021/jo202054g

Niphakis, M.J.; Gay, B.C.; Hong, K.H.; Bleeker, N.P.; Georg, G.I. Synthesis and evaluation of the anti-proliferative and NF-kB activities of a library of simplified tylophorine analogs. Bioorg. Med. Chem. 2012, 20, 5893-5900. DOI: 10.1016/j.bmc.2012.07.044

Sajjad, M.; Riaz, U.; Yao, R.; Bernacki, R. J.; Abouzied, M.; Erb, D. A.; Chaudhary, N. D.; Veith, J. M.; Georg, G. I.; Nabi, H. A. Investigation of 3'-Debenzoyl-3'-(3-([124I]-Iodobenzoyl)paclitaxel Analogues as Radio-tracers to Study Multidrug Resistance in vivo. Appl. Radiat. Isotopes 2012, 70, 1624-1631. DOI: 10.1016/j.apradiso.2012.03

2011

Bi, L.; Georg, G.I. Direct Hiyama cross-coupling of enaminones with triethoxy(aryl)silanes and dimethylphenylsilanol. Org. Lett. 2011, 13, 5413-5415. DOI: 10.1021/ol202202a *Featured as Synfacts-Article: Synfacts 01/12*

Betzi, S.; Alam, R.; Martin, M.; Lubbers, D.J.; Han, H.; Jakkaraj, S.R.; Georg, G.I.; Schonbrunn, E. Discovery of a potential allosteric ligand binding site in CDK2. ACS Chem. Biol. 2011, 6, 492-501. DOI: 10.1021/cb100410m

Leighty, M.W.; Spletstoser, J.T.; Georg, G.I. Mild conversion of tertiary amides to aldehydes using Cp2Zr(H)Cl (Schwartz's reagent). Org. Syn. 2011, 88, 427-437. DOI: 10.1002/0471264229.os088.39 *Featured Article on Organic Syntheses website (http://www.orgsyn.org/)*

Yu, Y-Y.; Niphakis, M.J.; Georg, G.I. Palladium(II)-catalyzed dehydrogenative alkenylation of cyclic enaminones via the Fujiwara-Moritani Reaction. Org. Lett. 2011, 13, 5932-5935. DOI: 10.1021/ol202677g

Pepe, A.; Pamment, M.; Georg, G.I.; Malhotra, S.V. Synthesis of fused bicyclic systems with nitrogen atom at the bridgehead, including indolizidines and quinolizidines. J. Org. Chem. 2011, 76, 3527-3530. DOI: 10.1021/jo102558u

Schneider, C.M.; Khownium, K.; Li, W.; Spletstoser, J.T.; Haack, T.; Georg, G.I. Synthesis of oximidine II by a copper-mediated reductive ene-yne macrocyclization. Angew. Chem. Int. Ed. 2011, 50, 7855-7857. DOI: 10.1002/anie.201103081 *Highlighted in Organic Chemistry Portal: www.organic-chemistry.org/Highlights/2012/09April.shtm*

Niphakis, M.J.; Georg, G.I. Synthesis of tylocrebrine and related phenanthroindolizidines by VOF3-mediated oxidative aryl-alkene coupling. Org. Lett. 2011, 13, 196-199. DOI: 10.1021/ol1023954

Doan, T.L.; Pollastri, M.; Walters, M.A.; Georg, G.I. The future of drug repositioning: old drugs, new opportunities. Annu. Rep. Med. Chem. 2011, 46, 385-401. DOI: 10.1016/B978-0-12-386009-5.00004-7

Seki, H.; Georg, G.I. Three-component synthesis of cyclic enaminones via ketene cyclization. Org. Lett. 2011, 13, 2147-2149. DOI: 10.1021/ol200358h

Leighty, M.W.; Georg, G.I. Total syntheses and cytotoxicity of (R)- and (S)-Boehmeriasin A. ACS Med. Chem. Lett. 2011, 2, 313-315. DOI: 10.1021/ml1003074

2010

Seki, H.; Georg, G. I. Synthesis of Amino Acid Derived Enaminones via Wolff Rearrangement Using Vinylogous Amides as Carbon Nucleophiles. J. Am. Chem. Soc. 2010, 132, 15512-15513. DOI: 10.1021/ja107329k *Featured in “New Synthesis”, Journal of Synthetic Organic Chemistry JAPAN, 2011, 69, 453.* *Featured as Synfacts-Article: Synfact1 2011, 711.*

Niphakis, M. J.; Georg, G. I. Total Syntheses of Arylindolizidine Alkaloids (+)-Ipalbidine and (+)-Antofine. J. Org. Chem. 2010, 75, 6019-6022. DOI: 10.1021/jo101051w

Niphakis, M. J.; Turunen, B. J.; Georg, G. I. Synthesis of 6- and 7-Membered Cyclic Enaminones: Scope and Mechanism. J. Org. Chem. 2010, 75, 6793-6805. DOI: 10.1021/jo100907u

Hemenway, J. N.; Jarho, P.; Henri, J. T.; Nair, S. K.; Vander Veide, D.; Georg, G. I.; Stella, V. J. Preparation and physicochemical characterization of a novel water-soluble prodrug of carbamazepine. J. Pharm. Sci. 2010, 99, 1810-1825. DOI: 10.1002/jps.21952

Reiff, E. A.; Nair, S. K.; Henri, J. T.; Greiner, J. F.; Reddy, B. S.; Chakrasali, R.; David, S. A.; Ting-Lan; Amin, E. A.; Himes, R. H.; Vander Veide, D.; Georg, G. I. Total Synthesis and Evaluation of C26-Hydroxyepothilone D Derivatives for Photoaffinity Labeling of β-Tubulin. J. Org. Chem. 2010, 75, 86-94. DOI: 10.1021/jo901752v

2009 

Ward, T. R.; Turunen, B. J.; Haack, T.; Neuenswander, B.; Chadrick, W.; Georg, G. I. Synthesis of a quinolone library from ynones. Tet. Lett. 2009, 50, 6494-6497. DOI: 10.1016/j.tetlet.2009.09.024

Desino, K. E.; Ansar, S.; Georg, G. I.; Himes, R. H.; Michaelis, M. L.; Powell, D. R.; Reiff, E. A.; Telikepalli, H.; Aldus, K. L. (3R,5S,7as)-(3,5-Bis(4-fluorophenyl)tetrahydro-1H-oxazolo[3,4-c]oxazol-7a-yl)methanol, a Novel Neuroprotective Agent. J. Med. Chem. 2009, 52, 7537-7543. DOI: 10.1021/jm900254k

Hutt, O. E.; Inagaki, J.; Reddy, B. S.; Nair, S. K.; Reiff, E. A.; Henri, J. T.; Greiner, J. F.; Vander Veide, D. G.; Ghiu, T.; Amin, E.A.; Himes, R. H.; Georg, G. I. Total synthesis and evaluation of 22-(3-azidobenzoyloxy)methyl epothilone C for photoaffinity labeling of β-tubulin. Bioorg. Med. Chem. Lett. 2009, 19, 3293-3296. DOI: 10.1016/j.bmcl.2009.04.077

Chakrabarti, S.; Svojanovsky, S. R.; Slavic, R.; Georg, G. I.; Wilson, G. S.; Smith, P. G. Artificial neural network-based analysis of high-throughput screening data improved for prediction of active compounds. J. Biomol. Screen. 2009, 14, 1236-1244. DOI: 10.1177/1087057109351312

Zhao, Y.; Bacher, A.; Illarionov, B.; Fischer, M.; Georg, G. I.; Ye, Q.; Fanwick, P. E.; Franzblau, S. G.; Wan, B.; Cushman, M. Discovery and Development of the Covalent Hydrates of Trifluoromethylated Pyrazoles as Riboflavin Synthase Inhibitors with Antibiotic Activity Against Mycobacterium tuberculosis. J. Org. Chem. 2009, 74, 5297-5303. DOI: 10.1021/jo900768c

Talukdar, A.; Breen, M.; Bacher, A.; Illarionov, B.; Fischer, M.; Georg, G. I.; Ye, Q.; Cushman, M. Discovery and Development of a Small Molecule Library with Lumazine Synthase Inhibitory Activity. J. Org. Chem.2009, 74, 5121-5134. DOI: 10.1021/jo900238q

2008

Turunen, B. J.; Ge, H.; Oyetunji, J.; Desino, K.E.; Vasandani, V.; Guethe, S.; Himes, R. H.; Audus, K. L.; Seelig, A.; Georg, G.I. Paclitaxel succinate analogs: Anionic and amide introduction as a strategy to impart blood-brain barrier permeability. Bioorg. Med. Chem. Lett. 2008, 18, 5971-5974. DOI: 10.1016/j.bmcl.2008.09.103

Ge, H.; Wang, J.; Kayser, M. M.; Himes, R. H.; Georg, G. I. Synthesis, tubulin assembly, and antiproliferative activity against MCF7 and NCI/ADR-RES cancer cells of 10-O- acetyl-5'-hydroxybutitaxel. Bioorg. Med. Chem. Lett. 2008, 18, 6165-6167. DOI: 10.1016/j.bmcl.2008.10.010

Hutt, O. E.; Reddy, B. S.; Nair, S. K.; Reiff, E. A.; Henri, J. T.; Greiner, J. F.; Chiu, T.; Vander Velde, D. G.; Amin, E. A.; Himes, R. H.; Georg, G. I. Total synthesis and evaluation of C25-benzyloxyepothilone C for tubulin assembly and cytotoxicity against MCF-7 breast cancer cells. Bioorg. Med. Chem. Lett. 2008, 18, 4904-4906. DOI: 10.1016/j.bmcl.2008.07.024

Kimball, S.F.; Himes, R. H.; Georg, G.I. Synthesis and evaluation of heteroaromatic 6,7-diaryl-2,3,8,8a-tetrahydroindolizin-5(1H)-ones for cytotoxicity against the HCT-116 colon cancer cell line. Bioorg. Med. Chem. Lett. 2008, 18, 3248-3250. DOI: 10.1016/j.bmcl.2008.04.051

Tash, J. S.; Attardi, B.; Hild, S. A.; Chakrasali, R.; Jakkaraj, S. R.; Georg, G. I. A novel potent indazole carboxylic acid derivative blocks spermatogenesis and is contraceptive in rats after a single oral dose. Biol. Reprod. 2008, 78, 1127-1138. DOI: 10.1095/biolreprod.106.057810

Tash, J. S.; Chakrasali, R.; Jakkaraj, S. R.; Hughes, J.; Smith, S. K.; Hornbaker, K.; Heckert, L. L.; Ozturk, S. B.; Hadden, M. K.; Kizzy, T. G.; Blagg, B. S.; Georg, G. I. Gamendazole, an orally active indazole carboxylic acid male contraceptive agent, targets HSP90AB1 (HSP90BETA) and EEF1A1 (eEF1A), and stimulates IL1a transcription in rat Sertoli cells. Biol. Reprod. 2008, 78, 1139-1152. DOI: 10.1095/biolreprod.107.062679

Vedantham, P.; Guerra, J. M.; Schoenen, F.; Huang, M.; Gor, P. J.; Georg, G. I.; Want, J. L.; Neuenswander, B.; Lushington, G. H.; Kitschier, L. A.; Ye, Q. Z.; Hanson, P. R. Ionic immobilization, diversification, and release: Application to the generation of a library of methionine aminopeptidase inhibitors. J. Comb. Chem. 2008, 10, 185-194. DOI: 10.1021/cc700085c

Santhapuram, H. K. R.; Datta, A.; Hutt, O. E.; Georg, G. I. N-Methylation of the C3' Amide of Taxanes: Synthesis of N-Methyltaxol C and N-Methylpaclitaxel. J. Org. Chem. 2008, 73, 4705-4708. DOI: 10.1021/jo800173h

Ge, H.; Niphakis, M. J.; Georg, G. I. Palladium (II)-Catalyzed Directed Acylation of Enaminones Using Organotrifluoroborates. J. Am. Chem. Soc. 2008, 130, 3708-3709. DOI: 10.1021/ja710221c

Vedantham, P.; Zhang, M.; Gor, P. J.; Huang, M.; Georg, G. I.; Lushington, G. H.; Mischer, L. A.; Ye, Q.; Hanson, P. R. Studies Towards the Synthesis of Methionine Aminopeptidase Inhibitors: Diversification Utilizing a ROMP-Derived Coupling Reagent. J. Comb. Chem. 2008, 10, 195-203. DOI: 10.1021/cc7000869

Kimball, F. S.; Turunen, B. J.; Ellis, K. C.; Himes, R. H.; Georg, G. I. Enantiospecific synthesis and cytotoxicity of 7-(4-methoxyphenyl)-6-phenyl-2,3,8,8a-tetrahydroindolizin-5(1H)-one enantiomers. Bioorg. Med Chem. 2008, 16, 4367-4377. DOI: 10.1016/j.bmc.2008.02.073

2007 

Wang, X.; Turunen, B. J.; Leighty, M. W.; Georg, G. I. Microwave-assisted Suzuki-Miyaura couplings on alpha-iodoenaminones. Tet. Lett. 2007, 48, 8811-8814. DOI: 10.1016/j.tetlet.2007.10.078

Kimball, F. S.; Tunoori, A. R.; Victory, S. F.; Dutta, D.; White, J. M.; Himes, R. H.; Georg, G. I. Synthesis, in vitro and in vivo cytotoxicity of 6,7-diaryl-2,3,8,8a-tetrahydroindolizin-5(1H)-ones. Bioorg. Med. Chem. Lett. 2007, 17, 4703-4707. DOI: 10.1016/j.bmcl.2007.05.103

Fried, Kristian, W.; Schneider, C. M.; Schramm, K.; Datta, A.; Chahbane, N.; Carsten, C.; Powell, D. R.; Lenoir, D.; Kettrup, A.; Terranova, P.; Georg, G. I.; Rozman, K. K. From dioxin to drug lead - the development of 2,3,7,8-tetrachlorophenothiazine. Chem. Med. Chem. 2007, 2, 890-897. DOI: 10.1002/cmdc.200700005

Dutta, D.; Datta, A.; Vander Velde, D. G.; Georg, G. I. Oxidation of baccatin III at C14. A facile rearrangement of the baccatin III core. Lett. Org. Chem. 2007, 4, 151-154. DOI: 10.2174/157017807780737246

Zhang, Y.; Illarionov, B.; Bacher, A.; Fischer, M.; Georg, G. I.; Ye, Q.; Vander Velde, D.; Fanwick, P. E.; Song, Y.; Cushman, M. A Novel Lumazine Synthase Inhibitor Derived from Oxidation of 1,3,6,8-Tetrahydroxy-2,7-naphthyridine to a Tetraazaperylenehexaone Derivative. J. Org. Chem. 2007, 72, 2769-2776. DOI: 10.1021/jo062246d

Spletstoser, J. T.; White, J. M.; Tunoori, A. R.; Georg, G. I. Mild and Selective Hydrozirconation of Amides to Aldehydes Using Cp2Zr(H)Cl: Scope and Mechanistic Insight. J. Am. Chem. Soc. 2007, 129, 3408-3419. DOI: 10.1021/ja066362+

Ge, H.; Spletstoser, J. T.; Yang, Y.; Kayser, M.; Georg, G. I. Synthesis of Docetaxel and Butitaxel Analogues through Kinetic Resolution of Racemic β-Lactams with 7-O-Triethylsilylbaccatin III. J. Org. Chem. 2007, 72, 756-759. DOI: 10.1021/jo061339s

Ahn, Y. M.; Vogtei, L.; Liu, C.; Santhapuram, H. K. R.; White, J. M.; Vasandani, V.; Mischer, L. A.; Lushington, G. H.; Paul, R.; Powell, D. R.; Times, R. H.; Ruby, K. F.; Ye, Q.; Georg, G. I. Design, synthesis, and antiproliferative and CDK2-cyclin a inhibitory activity of novel flavopiridol analogues. Bioorg. Med. Chem. 2007, 15, 702-713. DOI: 10.1016/j.bmc.2006.10.063

2006 

Turunen, B. J.; Georg, G. I. Amino Acid-Derived Enaminones: A Study in Ring Formation Providing Valuable Asymmetric Synthons. J. Am. Chem. Soc. 2006, 128, 8702-8703. DOI: 10.1021/ja0609046

Blackman, B.; Georg, G. I.; Lushington, G. H. CoMSIA/QSAR models for vacuolar (H+) ATPase inhibition by selected benzoate and benzolactone species. Lett. Drug Des. Discov. 2006, 3, 104-107. DOI: 10.2174/157018006775789748

Fang, J.; Dong, Y.; Lushington, G. H.; Ye, Q.; Georg, G. I. Support vector machines in HTS data mining: type I MetAPs inhibition study. J. Biomol. Screen. 2006, 11, 138-144. DOI: 10.1177/1087057105284334

Khownium, K.; Wood, S. J.; Miller, K. A.; Balakrishna, R.; Nguyen, T. B.; Kimbrell, M. R.; Georg, G. I.; David, S. A. Novel endotoxin-sequestering compounds with terephthalaldehyde-bis-guanylhydrazone scaffolds. Bioorg. Med. Chem. Lett. 2006, 16, 1305-1308. DOI: 10.1016/j.bmcl.2005.11.059

Spletstoser, J. T.; Turunen, B. J.; Desino, K.; Rice, A.; Datta, A.; Dutta, D.; Huff, J. K.; Himes, R. H.; Audus, K. L.; Seelig, A.; Georg, G. I. Single-site chemical modification at C10 of the baccatin III core of paclitaxel and Taxol C reduces P-glycoprotein interactions in bovine brain microvessel endothelial cells. Bioorg. Med. Chem. Lett. 2006, 16, 495-498. DOI: 10.1016/j.bmcl.2005.10.063

Ge, H.; Vasandani, V.; Huff, J. K.; Audus, K. L.; Himes, R. H.; Seelig, A.; Georg, G. I. Synthesis and interactions of 7-deoxy-, 10-deacetoxy, and 10-deacetoxy-7-deoxypaclitaxel with NCI/ADR-RES cancer cells and bovine brain microvessel endothelial cells. Bioorg. Med. Chem. Lett. 2006, 16, 433-436. DOI: 10.1016/j.bmcl.2005.09.043

2005

Michaelis, M. L.; Ansar, S.; Chen, Y.; Reiff, E. R.; Seyb, K. I.; Himes, R. H.; Aldus, K. L.; Georg, G. I. β-Amyloid-induced neurodegeneration and protection by structurally diverse microtubule-stabilizing agents. J. Pharm. Exp. Ther. 2005, 312, 659-668. DOI: 10.1124/jpet.104.074450

Haack, K. L.; Ahn, Y. M.; Georg, G. I. A convenient method to remove ruthenium byproducts from olefin metathesis reactions using polymer-bound triphenylphosphine oxide (TPPO). Mol. Divers. 2005, 9, 301-303. DOI: 10.1007/s11030-005-2480-6

Chen, J.; Illarionov, B.; Bacher, A.; Fischer, M.; Haase, I.; Georg, G. I.; Ye, Q.; Ma, Z.; Cushman, M. A high-throughput screen utilizing the fluorescence of riboflavin for identification of lumazine synthase inhibitors. Anal. Biochem. 2005, 338, 124-130. DOI: 10.1016/j.ab.2004.11.033

Rice, A.; Liu, Y.; Michaelis, M. L.; Himes, R. H.; Georg, G. I.; Audus, K. L. Chemical Modification of Paclitaxel (Taxol) Reduces P-Glycoprotein Interactions and Increases Permeation across the Blood-Brain Barrier in Vitro and in Situ. J. Med. Chem. 2005, 48, 832-838. DOI: 10.1021/jm040114b

Beck, Z. Q.; Aldrich, C. C.; Megarvey, N. A.; Georg, G. I.; Sherman, D. H. Chemoenzymatic Synthesis of Cryptophycin/Arenastatin Natural Products. Biochem. 2005, 44, 13457-13466. DOI: 10.1021/bi051140u

Haack, T.; Haack, K.; Diederich, W. E.; Blackman, B.; Roy, S.; Pusuluri, S.; Georg, G. I. Formal Total Syntheses of the (-)-Salicylihalamides A and B From D-Glucose and L-Rhamnose. J. Org. Chem. 2005, 70, 7592-7604. DOI: 10.1021/jo050750x

2004 

White, J. M.; Tunoori, A. R.; Turunen, B. J. Georg, G. I. [Bis(2-methoxyethyl)amino]sulfur trifluoride, the Deoxo-Fluor reagent: application toward one-flask transformations of carboxylic acids to amides. J. Org. Chem. 2004, 69, 2573-2576. DOI: 10.1021/jo035658k

Spletstoser, J. T.; White, J. M.; Georg, G. I. One-step facile synthesis of deuterium-labeled aldehydes from tertiary amides using Cp2Zr(D)Cl. Tet. Lett. 2004, 45, 2787-2789. DOI: 10.1016/j.tetlet.2004.02.030

Reiff, E. A.; Nair, S. K.; Reddy, B. S. N.; Inagaki, J.; Henri, J. T.; Greiner, J. F.; Georg, G. I. Practical syntheses of the C12-C21 epothilone subunit via catalytic asymmetric reductions: Itsuno-Corey oxazaborolidine reduction and asymmetric Noyori hydrogenation. Tet. Lett. 2004, 45, 5845-5847. DOI: 10.1016/j.tetlet.2004.06.009

Tripathy, N. K.; Georg, G. I. RCM approach for the total synthesis of crptophycin-24 (Arenastatin A). Tet. Lett. 2004, 45, 5309-5311. DOI: 10.1016/j.tetlet.2004.04.164

Spletstoser, J. T.; Flaherty, P. T.; Himes, R. H.; Georg, G. I. Synthesis and Anti-Tubulin Activity of a 3'-(4-Azidophenyl)-3'-dephenylpaclitaxel Photoaffinity Probe. J. Med. Chem. 2004, 47, 6459-6465. DOI: 10.1021/jm030581d

Barboni, L.; Giarlo, G.; Ricciutelli, M.; Baldini, R.; Georg, G. I.; Vander Velde, D. G.; Himes, R. H.; Wang, M.; Lakdawala, A.; Snyder, J. P. Synthesis, Modeling, and Anti-Tubulin Activity of a D-Seco Paclitaxel Analogue. Org. Lett. 2004, 6, 461-464. DOI: 10.1021/ol036204c

Buck, S. B.; Huff, J. K.; Himes, R. H.; Georg, G. I. Total Synthesis and Anti-Tubulin Activity of Epi-C3 Analogues of Cryptophycin-24. J. Med. Chem. 2004, 47, 3697-3699. DOI: 10.1021/jm030555f

2003 

Haack, T.; Kurtkaya, S.; Snyder, J. P.; Georg, G. I. Studies toward the Synthesis of Oximidines I and II. Org. Lett. 2003, 5, 5019-5022. DOI: 10.1021/ol036007d

Yang, K.; Blackman, B.; Diederich, W.; Flaherty, P. T.; Mossman, C. J.; Roy, S.; Ahn, Y. M.; Georg, G. I. Formal Total Synthesis of (+)-Salicylihalamides A and B: A Combined Chiral Pool and RCM Strategy. J. Org. Chem. 2003, 68, 9687-9693. DOI: 10.1021/jo0301550

Vidya, R.; Eggen, M.; Nair, S. K.; Georg, G. I.; Himes, R. H. Synthesis of cryptophycins via an N-acyl-β-lactam macrolactonization. J. Org. Chem. 2003, 68, 9687-9693. DOI: 10.1021/jo0302197

Rice, A.; Michaelis, M. L.; Georg, G. I.; Liu, Y.; Turunen, B.; Audus, K. L. Overcoming the blood-brain barrier to taxane delivery for neurodegenerative diseases and brain tumors. J. Mol. Neurosci. 2003, 20, 339-343.

Yang, K.; Haack, T.; Blackman, B.; Diederich, W. E.; Roy, S.; Pusuluri, S.; Georg, G. I. Enantiospecific Formal Total Syntheses of (-)-Salicylihalamides A and B from D-Glucose and L-Rhamnose. Org. Lett. 2003, 5, 4007-4009. DOI: 10.1021/ol035630v

Gupta, M. L.; Bode, C. J.; Georg, G. I.; Himes, R. H. Understanding tubulin-taxol interactions: Mutations that impart taxol binding to yeast tubulin. Proc. Nat. Acad. Sci. 2003, 100, 6394-6397. DOI: 10.1073/pnas.1131967100

Vidya, R.; Eggen, M.; Georg, G. I.; Himes, R. H. Cryptophycin affinity labels: synthesis and biological activity of a benzophenone analogue of cryptophycin-24. Bio. Org. Med. Chem. Lett. 2003, 13, 757-760. DOI: 10.1016/S0960-894X(02)01023-5

Li, G.; Faibushevich, A.; Turunen, B. J.; Yoon, S. O.; Georg, G. I.; Michaelis, M. L.; Dobrowsky, R. T. Stabilization of the cyclin-dependent kinase 5 activator, p35, by paclitaxel decreases β-amyloid toxicity in cortical neurons. J. Neurochem. 2003, 84, 347-362. DOI: 10.1046/j.1471-4159.2003.01526.x

2002

Gao, X.; Petroff, B. K.; Oluola, O.; Georg, G. I.; Terrnova, P. F.; Rozman, K. K. Endocrine disruption by indole-3-carbinol and tamoxifen: blockage of ovulation. Toxicol. Appl. Pharm. 2002, 183, 179-188. DOI: 10.1006/taap.2002.9478

Michaelis, M. L.; Chen, Y.; Hill, S.; Reiff, E.; Georg, G. I.; Rice, A.; Audus, K. Amyloid peptide toxicity and microtubule-stabilizing drugs. J. Mol. Neurosci. 2002, 19, 101-105. DOI: 10.1007/Fs12031-002-0018-2

Ahn, Y. M.; Vander Velde, D. G.; Georg, G. I. Synthetic Studies with 13-Deoxybaccatin III. J. Org. Chem. 2002, 67, 7140-7143. DOI: 10/1021/jo011183q

Eggen, M. J.; Georg, G. I. The cryptophycins: Their synthesis and anticancer activity. Med. Res. Rev. 2002, 22, 85-101. DOI: 10.1002/med.10002

Liu, Y.; Ali, S. M.; Boge, T. C.; Georg, G. I.; Victory, S.; Zygmunt, J.; Marquez, R. T.; Himes, R. H. A systematic SAR study of C10 modified paclitaxel analogues using a combinatorial approach. Comb. Chem. High Throughput Screen. 2002, 5, 39-48. DOI: 10.2174/1386207023330615

Bode, C. J.; Gupta, M. L.; Reiff, E. A.; Suprenant, K. A.; Georg, G. I.; Himes, R. H. Epothilone and paclitaxel: unexpected differences in promoting the assembly and stabilization of yeast microtubules. Biochem. 2002, 41, 3870-3874. DOI: 10.1021/bi0121611

2001 

Reddy, S. H. K.; Lee, S.; Datta, A.; Georg, G. I. Efficient Synthesis of the 3'-Phenolic Metabolite of Paclitaxel. J. Org. Chem. 2001, 66, 8211-8214. DOI: 10.1021/jo0102516

Eggen, M. J.; Nair, S. K.; Georg, G. I. Rapid Entry into the Cryptophycin Core via an Acyl-β-lactam Macrolactonization: Total Synthesis of Cryptophycin-24. Org. Lett. 2001, 3, 1813-1815. DOI: 10.1021/ol010044s

Barboni, L.; Datta, A.; Dutta, D.; Georg, G. I.; Van der Velde, D. G.; Himes, R. H.; Wang, M.; Snyder, J. P. Novel D-Seco Paclitaxel Analogues: Synthesis, Biological Evaluation, and Model Testing. J. Org. Chem.2001, 66, 3321-3329. DOI: 10.1021/jo0015467

Ahn, Y. M.; Yang, K.; Georg, G. I. A Convenient Method for the Efficient Removal of Ruthenium Byproducts Generated during Olefin Metathesis Reactions. Org. Lett. 2001, 3, 1411-1413. DOI: 10.1007/s11030-005-2480-6

Georg, G. I.; Ahn, Y. M.; Blackman, B.; Farokhi, F.; Flaherty, P. T.; Mossman, C. J.; Roy, S.; Yang, K. Short and efficient chiral pool and RCM approach towards the synthesis of the macrocyclic core of the salicylihalamides. Chem. Comm. 2001, 3, 255-266. DOI: 10.1039/B008842K

2000 

White, J. M.; Tunoori, A. R.; Georg, G. I. A Novel and Expeditious Reduction of Tertiary Amides to Aldehydes Using Cp2Zr(H)Cl. J. Am. Chem. Soc. 2000, 122, 11995-11996. DOI: 10.1021/ja002149g

Tunoori, A. R.; White, J. M.; Georg, G. I. A One-Flask Synthesis of Weinreb Amides from Chiral and Achiral Carboxylic Acids Using the Deoxo-Fluor Fluorinating Reagent. Org. Lett. 2000, 2, 4091-4093. DOI: 10.21/ol000318w

Eggen, M; Mossman, C. J.; Buck, S. B.; Nair, S. K.; Bhat, L.; Ali, S. M.; Reiff, E. A.; Boge, T. C.; Georg, G. I. Total Synthesis of Cryptophycin-24 (Arenastatin A) Amenable to Structural Modifications in the C16 Side Chain. J. Org. Chem. 2000, 65, 7792-7799. DOI: 10.1021/jo000767+

1999 

Dutta, D.; Hadd, H.; Van der Velde, D. G.; Georg, G. I. A one-step synthesis of a deuterated paclitaxel analogue: 10-deacetoxy-(10α-2H)paclitaxel. Bioorg. Med. Chem. Lett. 1999, 9, 3277-3278. DOI: 10.1016/S0960-894X(99)00609-5

Boge, T. C.; Wu, Z.; Himes, R. H.; Van der Velde, D. G.; Georg, G. I. Conformationally restricted paclitaxel analogues: macrocyclic mimics of the "hydrophobic collapse" conformation. Bioorg. Med. Chem. Lett.1999, 9, 3047-3052. DOI: 10.1016/S0960-894X(99)00522-3

Boge, T. C.; Hepperle, M.; Van der Velde, D. G.; Gunn, C. W.; Grunewald, G. L.; Georg, G. I. The oxetane conformational lock of paclitaxel: structural analysis of D-secopaclitaxel. Bioorg. Med. Chem. Lett. 1999, 9, 3041-3046. DOI: 10.1016/S0960-894X(99)00521-1

Krise, J. P.; Zygmunt, J.; Georg, G. I.; Stella, V. J. Novel Prodrug Approach for Tertiary Amines: Synthesis and Preliminary Evaluation of N-Phosphonooxymethyl Prodrugs. J. Med. Chem. 1999, 42, 3094-3100. DOI: 10.1021/jm980539w

1998 

Bhat, L.; Liu, Y.; Victory, S. F.; Himes, R. H.; Georg, G. I. Synthesis and evaluation of paclitaxel C7 derivatives: solution phase synthesis of combinatorial libraries. Bioorg. Med. Chem. Lett. 1998, 8, 3181-3186. DOI: 10.1016/S0960-894X(98)00551-4

Eggen, M.; Georg, G. I. Enantioselective synthesis of a 3'-dephenylcryptophycin synthon. Bioorg. Med. Chem. Lett. 1998, 8, 3177-3180. DOI: 10.1016/S0960-894X(98)00557-5

Tunoori, A. R.; Dutta, D.; Georg, G. I. Polymer-bound triphenylphosphine as traceless reagent for Mitsunobu reactions in combinatorial chemistry: synthesis of aryl ethers from phenols and alcohols. Tet. Lett. 1998, 39, 8751-8754. DOI: 10.1016/S0040-4039(98)01988-1

Georg, G. I.; Harriman, G. C. B.; Datta, A.; Ali, S.; Cheruvallath, Z.; Dutta, D.; Van der Velde, D. G.; Himes, R. H. The Chemistry of the Taxane Diterpene: Stereoselective Reductions of Taxanes. J. Org. Chem.1998, 63, 8926-8934. DOI: 10.1021/jo981194s

Georg, G. I.; Ali, S. M.; Stella, V. J.; Waugh, W. N.; Himes, R. H. Halohydrin analogs of cryptophycin 1: Synthesis and biological activity. Bioorg. Med. Chem. Lett. 1998, 8, 1959-1962. DOI: 10.1016/S0960-894X(98)00356-4

1997 

Georg, G. I.; Liu, Y.; Boge, T. C.; Himes, R. H. 7-O-Acylpaclitaxel analogs: potential probes to map the paclitaxel binding site. Bioorg. Med. Chem. Lett. 1997, 7, 1829-1832. DOI: 10.1016/S0960-894X(97)00329

Ali, S. M.; Georg, G. I. Formal syntheses of cryptophycin A and arenastatin A. Tet. Lett. 1997, 38, 1703-1706. DOI: 10.1016/S0040-4039(97)00194-9

Ali, S. M.; Hoemann, M. Z.; Aube, J.; Georg, G. I.; Mitscher, L. A.; Jayasinghe, L. R. Butitaxel Analogs: Synthesis and Structure-Activity Relationships. J. Med. Chem. 1997, 236-241. DOI: 10.1021/jm960505t

1996 

Park, H.; Hepperle, M.; Boge, T. C.; Himes, R. H.; Georg, G. I. Preparation of Phenolic Paclitaxel Metabolites. J. Med. Chem. 1996, 39, 2705-2709. DOI: 10.1021/jm960142x

Wu, Z.; Georg, G. I.; Cathers, B. E.; Schloss, J. V. Synthesis and evaluation of beta-lactam-containing dipeptide analog as a protease inhibitor. Bioorg. Med. Chem. Lett. 1996, 6, 983-986. DOI: 10.1016/0960-894X(96)00153-9

Victory, S. F.; Van der Velde, D. G.; Jalluri, R. K.; Grunewald, G. L.; Georg, G. I. Relative stereochemistry and solution conformation of the novel paclitaxel-like antimitotic agent epothilone A. Bioorg. Med. Chem. Lett. 1996, 6, 893-898. DOI: 10.1016/0960-894X(96)00139-4

Georg, G. I.; Harriman, G. C. B.; Hepperle, M.; Clowers, J. S.; Vander Velde, D. G.; Himes, R. H. Synthesis, Conformational Analylsis, and Biological Evaluation of Heteroaromatic Taxanes. J. Org. Chem. 1996, 61, 2664-2676. DOI: 10.1021/jo951961

1995

Kerksiek, K.; Mejillano, M. R.; Schwartz, R. E.; Georg, G. I.; Himes, R. H. Interaction of cryptophycin 1 with tubulin and microtubules. FEBS Lett. 1995, 377, 59-61. DOI: 10.1016/0014-5793(95)01271-0

Harriman, G. C. B.; Jalluri, R. K.; Grunewald, G. L.; Van der Velde, D. G.; Georg, G. I.; Himes, R. H. The chemistry of taxane diterpene: stereoselective synthesis of 10-deacetoxy-11,12-epoxypaclitaxel. Tet. Lett. 1995, 36, 8909-8912. DOI: 10.1016/0040-4039(95)01928-B

Georg, G. I.; Harriman, G. C. B.; Peterson, S. A. A Facile One-Flask Conversion of Aldehydes and Ketones to N-Sulfonyl Imines. J. Org. Chem. 1995, 60, 7366-7368. DOI: 10.1021/jo00127a054

Ali, S. M.; Hoemann, M. Z.; Aube, J.; Mitscher, L. A.; Georg, G. I.; McCall, R.; Jayasinghe, L. R. Novel cytotoxic 3'-(tert-Butyl) 3'-diphenyl analogs of paclitaxel and docetaxel. J. Med. Chem. 1995, 38, 3821-3828. DOI: 10.1021/jm00019a012

Sengupta, S.; Boge, T. C.; Georg, G. I.; Himes, R. H. Interaction of a fluorescent paclitaxel analog with tubulin. Biochem. 1995, 34, 11889-11894. DOI: 10.1021/bi00037a029

Hoemann, M. Z.; Van der Velde, D. G.; Aube, J.; Georg, G. I.; Jayasinghe, L. R. Synthesis of 13-epi-Taxol via a Transannular Delivery of a Borohydride Reagent. J. Org. Chem. 1995, 60, 2918-2921. DOI: 10.1021/jo000114a052

Datta, A.; Van der Velde, D. G.; Georg, G. I.; Himes, R. H. Syntheses of novel C-9 and C-10 modified bioactive taxanes. Tet. Lett. 1995, 36, 1985-1988. DOI: 10.1016/0040-4039(95)00208-T

Georg, G. I.; Boge, T. C.; Park, H.; Himes, R. H. Paclitaxel and docetaxel photoaffinity labels. Bioorg. Med. Chem. Lett. 1995, 5, 615-620. DOI: 10.1016/0960-894X(95)00083-6

Georg, G. I.; Cheruvallath, Z. S.; Van der Velde, D. G. Stereoselective synthesis of 9β-hydroxytaxanes via reduction with samarium diiodide. Tet. Lett. 1995, 36, 1783-1786. DOI: 10.1016/0040-4039(95)00142-Y

Georg, G. I.; Ali, S. M.; Boge, T. C.; Datta, A.; Aalborg, L.; Park, H. Synthesis of biologically active 2-benzoyl paclitaxel analogs. Bioorg. Med. Chem. Lett. 1995, 5, 259-264. DOI: 10.1016/0960-894X(95)00020-T

Georg, G. I.; Harriman, G. C. B.; Ali, S. M.; Datta, A.; Hepperle, M.; Himes, R. H. Synthesis of 2-O-heteroaroyl taxanes: evaluation of microtubule assembly promotion and cytotoxicity. Bioorg. Med. Chem. Lett.1995, 5, 115-118. DOI: 10.1016/0960-894X(94)00468-U

Datta, A.; Hepperle, M.; Georg, G. I. Selective Deesterification Studies on Taxanes: Simple and Efficient Hydrazinolysis of C-10 and C-13 Ester Functionalities. J. Org. Chem. 1995, 60, 761-763. DOI: 10.1012/jo00108a053

1994 

Georg, G. I.; Ali, S. M.; Boge, T. C.; Datta, A.; Aalborg, L.; Himes, R. H. Selective C-2 and C-4 deacylation and acylation of taxol: the first synthesis of a C-4 substituted taxol analog. Tet. Lett. 1994, 35, 8931-8934. DOI: 10.1016/0040-4039(94)88392-0

Datta, A.; Jayasinghe, L. R.; Georg, G. I. 4-Deacetyltaxol and 10-Acetyl-4-deacetyltaxotere: Synthesis and Biological Evaluation. J. Med. Chem. 1994, 37, 4258-4260. DOI: 10.1021/jm00050a023

Georg, G. I.; Cheruvallath, Z. S.; Harriman, G. C. B.; Hepperle, M.; Park, H.; Himes, R. H. Synthesis and biology of substituted 3'-phenyl taxol analogs. Bioorg. Med. Chem. Lett. 1994, 4, 2331-2336. DOI: 10.1016/0960-894X(94)00335-1

Datta, A.; Aube, J.; Georg, G. I.; Mitshcher, L. A.; Jayasinghe, L. R. The first synthesis of a C-9 carbonyl modified baccatin III derivative and its conversion to novel Taxol and Taxotere analogs. Bioorg. Med. Chem. Lett. 1994, 4, 1831-1834. DOI: 10.1016/S0960-894X(01)80379-6

Georg, G. I.; Boge, T. C.; Cheruvallath, Z. S.; Harriman, G. C. B.; Heuperle, M.; Park, H.; Himes, R. H. Topliss approach to the synthesis of biologically active substituted N-benzoyl taxol analogs. Bioorg. Med. Chem. Lett. 1994, 4, 1825-1830. DOI: 10.1016/S0960-894X(01)80378-4

Boge, T. C.; Himes, R. H.; Van der Velde, D. G.; Georg, G. I. The Effect of the Aromatic Rings of Taxol on Biological Activity and Solution Conformation: Synthesis and Evaluation of Saturated Taxol and Taxotere Analogs. J. Med. Chem. 1994, 37, 3337-3343. DOI: 10.1021/jm00046a018

Jayasinghe, L. R.; Datta, A.; Ali, S. M.; Zygmunt, J.; Van der Velde, D. G.; Georg, G. I. Structure-Activity Studies of Antitumor Taxanes: Synthesis of Novel C-13 Side Chain Homologated Taxol and Taxotere Analogs. J. Med. Chem. 1994, 37, 2981-2984. DOI: 10.1021/jm00044a020

Dasgupta, D.; Park, H.; Harriman, G. C. B.; Georg, G. I.; Himes, R. H. Synthesis of a Photoaffinity Taxol Analog and Its Use in Labeling Tubulin. J. Med. Chem. 1994, 37, 2976-2980. DOI: 10.1021/jm00044a019

Georg, G. I.; Harriman, G. C. B.; Hepperle, M.; Himes, R. H. Heteroaromatic taxol analogs: the chemistry and biological activities of 3'-furyl and 3'-pyridyl substituted taxanes. Bioorg. Med. Chem. Lett. 1994, 4, 1381-1384. DOI: 10.1016/S0960-894X(01)80366-8

Georg, G. I.; Cheruvallath, Z. S. Samarium Diiodide-Mediated Deoxygenation of Taxol: A One-Step Synthesis of 10-Deacetoxytaxol. J. Org. Chem. 1994, 59, 4015-4018. DOI: 10.1021/jo00093a040

Van der Velde, D. G.; Georg, G. I.; Gollapudi, S. R.; Jampani, H. B.; Liang, X.; Mitscher, L. A.; Ye, Q. Wallifoliol, a taxol congener with a novel carbon skeleton, from Himalayan Taxus wallichiana. J. Nat. Prod.1994, 57, 862-867. DOI: 10.1021/np50108a032

Georg, G. I.; Harriman, G. C. B.; Park, H.; Himes, R. H. Taxol photoaffinity labels. 2. Synthesis and biological evaluation of N-(4-azidobenzoyl)-N-debenzoyltaxol, N-(4-azido-2,3,5,6-tetrafluorobenzoyl)-N-debenzoyltaxol, and 7-(4-azido-2,3,5,6-tetrafluorobenzoyl)taxol. Bioorg. Med. Chem. Lett. 1994, 4, 487-490. DOI: 10.1016/0960-894X(94)80022-7

Datta, A.; Jayasinghe, L. R.; Georg, G. I. Internal Nucleophile Assisted Selective Deesterification Studies on Baccatin III. Synthesis of 2-Debenzoyl- and 4-Deacetylbaccatin III Analogs. J. Org. Chem. 1994, 59, 4689-4690. DOI: 10.1021/jo00095a055

Georg, G. I.; Boge, T. C.; Cheruvallath, Z. S.; Harriman, G. C. B.; Heuperle, M.; Park, H.; Himes, R. H. Schotten-Baumann acylation of N-debenzoyltaxol; an efficient route to N-acyl taxol analogs and their biological evaluation. Bio. Org. Med. Chem. Lett. 1994, 4, 335-338. DOI: 10.1016/S0960-894X(01)80139-6

Georg, G. I.; Wu, Z. An investigation of (R)-(+)-1-(1-naphthyl)ethylimines and (R)-(+)-1-(phenyl)ethylimines as chiral templates in the Staudinger reaction. Tet. Lett. 1994, 35, 381-384. DOI: 10.1016/0040-4039(94)85059-3

1993 

Georg, G. I.; Cheruvallath, Z. S.; Harriman, G. C. B.; Hepperle, M.; Park, H. An efficient semisynthesis of taxol from (3R,4S)-N-benzoyl-3-[test-butyldimethylsilyl)oxy]-4-phenyl-2-azetidinone and 7-(triethylsilyl)baccatin III. Bioorg. Med. Chem. Lett. 1993, 3, 2467-2470. DOI: 10.1016/S0960-894X(01)80979-3

Georg, G. I.; Gollapudi, S. R.; Grunewald, G. L.; Gunn, C. W.; Himes, R. H.; Rao, B. K.; Liang, X. Z.; Mirhom, Y. W.; Mitscher, L. A.; Van der Velde, D. G.; Ye, Q. A reinvestigation of the taxol content of Himalayan Taxus wallichiana Zucc. and a revision of the structure of brevifoliol. Bioorg. Med. Chem. Lett. 1993, 3, 1345-1348. DOI: 10.1016/S0960-894X(00)80345-5

Van der Velde, D. G.; Georg, G. I.; Grunewald, G. L.; Gunn, C. W.; Mitscher, L. A. "Hydrophobic collapse" of taxol and Taxotere solution conformations in mixtures of water and organic solvent. J. Am. Chem. Soc.1993, 115, 11650-11651. DOI: 10.1021/ja00077a095

Georg, G. I.; Cheruvallath, Z. S.; Van der Velde, D. G.; Ye, Q.; Mitscher, L. A.; Himes, R. H. Semisynthesis and biological evaluation of brevifoliol 13-[N-benzoyl-(2'R,3'S)-3'-phenylisoserinate]. Bioorg. Med. Chem. Lett. 1993, 3, 1349-1350. DOI: 10.16/S0960-894X(00)80346-7

Georg, G. I.; He, P.; Kant, J.; Wu, Z. J. Stereocontrolled synthesis of N-vinyl-, N-(1'-propenyl)-, and N-unsubstituted-β-lactams from 2-aza-1,3-butadienes via the Staudinger reaction. J. Org. Chem. 1993, 58, 5771-5778. DOI: 10.1021/jo00073a042