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Publications since Independent Career
Publications since Independent Career
48) Leveraging Conformational Control of Neratinib’s C–N Axes to Enhance HER4 selectivity in Ovarian Cancer. Beeta S. Heydaria, Megan A. Keenec, Bahar S. Heydaria, Madeline Rougiera, Alyssa A. Gomeza, Nicholas E. Fraschilla-Brodkinb, Carrie D. Housec, and Jeffrey L. Gustafson. Chemrxiv 2026 (Link)
47) Leveraging Atropisomerism to Obtain a Mutant-Selective c-KIT Inhibitor in Gastrointestinal Stromal Tumors. Bahar S. Heydaria, Diwakar Guragainc,d, Beeta S. Heydaria, Chih-Min Tangc,d, Julia V. Simonb, Andrew M. O’Brienb, Nilay Kanova Dogana, Angeline Philipa, Aaron Robertsa, Yuezhi Maoa, Jason K. Sicklickc,d, and Jeffrey L. Gustafsonb* Chemrxiv 2026 (Link)
46) "A Rh(II) Catalyzed Atropisomer Selective Ring Expansion of 3-Aryl Indoles to 4-Aryl Quinolines" Basilaia, Mi.§ ; Zanolini, R.§; Dogan, N.; Rustin, G.; Regganie, T.; Susskind, N.; Mao, Y.; Gustafson, J. ACS Catal. 2026, XXXX, XXX, XXX-XXX (Link)
45) "Trifluoromethylation of Arenes and Heterocycles via a Bench-Stable Photocaged Trifluoromethylation Reagent" Rustin, G.;... Taylor, M.; Gustafson, Org. Lett. 2025, 27, 49, 13504-13508 (Link)
44) “CySP3-96 enables scalable, streamlined, and low-cost sample preparation for cysteine chemoproteomic applications” Shikwana, F.; Heydari, B.; Ofori, S.; Truong, C.; Turmon, A.; Darrouj, J.; Holoidovsky, L; Gustafson, J.; Backus, K. Molecular & Cellular Proteomics 2024 (Link)
43) “Targeting the RET tyrosine kinase in neuroblastoma: A review and application of a novel selective drug design strategy” Steen, E.; Basilaia, M.; Kim, W.; Getz, T.; Gustafson, J. Biochemical Pharmacology. 2023, 216, 115751 (Link)
42) “A Light-Promoted Innate Trifluoromethylation of Pyridones and Related N-Heteroarenes.” Dang-Nguyen, A.; Legaspi, K. C.; McCarty, C. T.; Smith, D. K.; Gustafson, J. Org. Lett. 2023, 25, 26, 4898–4902 (Link)
41) “Controlling Ibrutinib’s Conformations about Its Heterobiaryl Axis to Increase BTK Selectivity.” Toenjes, S. T.; Heydari, B. S.; Albright, S. T.; Hazin, R.; Ortiz, M. A.; Piedrafita, J.; Gustafson, J. ACS Med. Chem. Lett. 2023. 14, 3, 305–311. (Link)
40) “Selective Functionalization of Arenes and Heteroarenes via SEAr and Related Transformations” Nguyen, A. D.; Zanolini, R. J,; Gustafson, J.L. Contributed chapter to book published by Wiley titled ‘Handbook of C-H Functionalization’. 2022. (Link)
39) “Atropisomerism in the Pharmaceutically Relevant Realm” Basilaia, M.; Chen, H. M.; Secka, J.; Gustafson, J. L. Acc. Chem. Res. 2022, 55, 20, 2904–2919 (Link)
38) “Approaches toward Atropisomerically Stable and Conformationally Pure Diarylamines” Vaidya, S. D.; Heydari, B. S.; Toenjes, S. T.; Gustafson, J. L. J. Org. Chem. 2022, 87, 10, 6760–6768 (Link)
37) “Catalytic Atroposelective Dynamic Kinetic Resolutions and Kinetic Resolutions towards 3-arylquinolines via SNAr ” Cardenas, M. C.; Saputra, M. A.; Gordon, D. A.; Sanchez, A. N.; Yamamoto, N.; Gustafson, J. L. Chem. Comm. 2021. (Link)
36) “Asymmetric Synthesis of Nonbiaryl Atropisomers” Saputra, M. A.; Cardenas, M. C.; Gustafson, J. L. Contributed chapter to book published by Wiley titled ‘Axially Chiral Compounds’. 2021. (Link)
ISBN:978-3-527-34712-4
35) “Atropisomerism as Inspiration For New Chemistry” Cardenas, M.; Nguyen, A. D.; Brown, Z.; Heydari, B.; Heydari, B.; Vaidya, S.; Gustafson, J. Arkivoc. 2021. i. 20-47 (Link)
34) “Leveraging conformational control about a potential atropisomeric axis as a strategy in medical chemistry” Toenjes, Sean T., Mariam Basilaia, and Jeffrey L. Gustafson, Future Med. Chem. 2021, 13(5), 443-446. (Link)
32) “Redox-Responsive H-Bonding: Amplifying the Effect of Electron Transfer Using Proton-Coupled Electron Transfer” Choi, H.; Baek, K.; Toenjes, S.; Gustafson, J.; Smith, D. J. Am. Chem. Soc., 2020. (Link)
31) “A Catalytic Cycle of Discovery: Asymmetric Catalysis Gives Rise to New Chiral Catalyst Scaffolds” Dinh, A. N. and Gustafson, J. L. Chem, 2020, 6 (4), 919-932. (Link)
30) “Discovery of Cyclic Guanidine-linked Sulfonamides as Inhibitors of LMTK3 kinase” Ortiz M. A.; Michaels, H.; Molina, B.; Toenjes, S.; Davis J.; Marconi G. D.; Hecht D.; Gustafson J. L.; Piedrafita, J. F.; Nefzi, A. Bioorganic & Medicinal Chemistry Letters 2020, 30 (9), 127108. (Link)
29) “Catalytic Atroposelective Synthesis of N-Aryl Quinoid Compounds” Vaidya, S. D.; Toenjes, S. T.; Yamamoto, N.; Maddox, S. M.; Gustafson J. L. J. Am. Chem. Soc., 2020, 142 (5), 2198-2203. (Link)
28) “Photocatalytic Oxidative C-H Thiolation: Synthesis of Benzothiazoles and Sulfenylated Indoles” Dinh, A. N.; Nguyen, A. D.; Millan Aceves, E.; Albright, S. T.; Cedano, M. R.; Smith, D. K.; Gustafson, J. L. Synlett 2019, 30 (14), 1648-1655 (Link).
27) “Leveraging atropisomerism to Obtain a Selective Inhibitor of RET kinase with Secondary Activities towards EGFR Mutants” Toenjes S. T.; Garcia, V.; Maddox, S. M.; Dawson, G.A.; Ortiz, M. A.; Piedrafita, J.; Gustafson, J.L. ACS Chem. Biol. 2019, 14 (9), 1930-1939. (Link)
26) “Toward a Catalytic Atroposelective Synthesis of Diaryl Ethers Through C(sp2)–H Alkylation with Nitroalkanes” Dinh, A. N.; Noorbehesht, R. R.; Toenjes, S. T.; Jackson, A. C.; Saputra, M. A.; Maddox, S. M.; Gustafson, J. L. Synlett. 2018. (doi: https://doi.org/10.1055/s-0037-1609581)
25) “Lewis Base/Bronsted Acid Dual-Catalytic C–H Sulfenylation of Aromatics” Nalbandian, C. J.; Brown, Z. E.; Alvarez, E.; Gustafson, J. L. Org Lett. 2018, 20 (11), 3211–3214. (doi: https://doi.org/10.1021/acs.orglett.8b01066)
24) “Enantioselective Synthesis of Biaryl Atropisomers via the Addition of Thiophenols into Aryl-Naphthoquinones” Maddox, S. M.; Dawson, G. A.; Rochester, N. C.; Ayonon, A. B.; Moore, C. E.; Rheingold, A. L; Gustafson. J. L. ACS Catal. 2018, 8, 5443–5447. (doi: https://doi.org/10.1021/acscatal.8b00906)
23) “Enantioselective Synthesis of Pyrrolopyrimidine Scaffolds through Cation-Directed Nucleophilic Aromatic Substitution” Cardenas, M. M.; Toenjes, S. T.; Nalbandian, C. J.; Gustafson, J. L. Org. Lett. 2018, 20, 2037-2041. (doi: https://doi.org/10.1021/acs.orglett.8b00579)
22) “Atropisomerism in medicinal chemistry: challenges and opportunities” Toenjes, S. T.; Gustafson, J. L. Future Med. Chem. 2018, 10(4), 409-422. (doi: https://doi.org/10.4155/fmc-2017-0152)
21) “Benzylic bromination catalyzed by triphenylphosphine selenide via Lewis basic activation” Ayonon, A; Nalbandian, C. J.; Guillemard, L.; Gustafson, J. L. Tetrahedron Lett. 2017, 58, 2940-2943. (doi: https://doi.org/10.1016/j.tetlet.2017.06.042)
20) “A conjugate Lewis base-Brønsted acid catalyst for the sulfenylation of nitrogen containing heterocycles under mild conditions” Nalbandian, C. J.; Miller, E. M.; Toenjes, S. T.; Gustafson, J. L. Chem. Commun. 2017, 53, 1494-1497. (doi: https://doi.org/10.1039/C6CC09998J)
19) “The Catalyst Controlled Regiodivergent Chlorination of Phenols” Maddox, S. M.; Dinh, A, N.; Armenta, F.; Um, J.; Gustafson, J. L. Org. Lett. 2016, 18, 5476. [Highlighted in Synfacts, Jan 2017], (doi: https://doi.org/10.1021/acs.orglett.6b02650)
18) “Water mediated Wittig Reactions of Aldehydes in the teaching laboratory: using sodium Bicarbonate for the in situ formation of stabilized ylides” Kelley, M. J. B.; Fallot, L. B.; Gustafson, J. L.; Bergdahl, B. M. J. Chem. Ed. 2016, 93, 1631-1636. (doi: https://doi.org/10.1021/acs.jchemed.6b00206)
17) “Enhancing the selectivity of kinase inhibitors in oncology: A Chemical Biology Perspective” Maddox, S. M.; Hecht, D. E.; Gustafson, J. L. Future Med. Chem. 2016, 8, 241-244. (doi: https://doi.org/10.4155/fmc.15.193)
16) “The preorganization of Atropisomers to Increase target Selectivity.” Nalbandian, C. J.; Hecht, D. E.; Gustafson, J. L.; Syn. Lett. 2016, 27, 977-983. (doi: https://doi.org/10.1055/s-0035-1561314)
15) “Exploiting Atropisomerism to Increase the Target Selectivity of Kinase Inhibitors” Smith, D. E.; Marquez, I.; Lokensgard, M.; Rheingold, A. L, Hecht, D.; Gustafson, Jeffrey L. Angew. Chem. Int. Ed., 2015, 54, 11754-11759.[This paper was highlighted in numerous journals including ACS Chem Bio, Synthetic Letters and Future Medicinal Chemistry] (doi: https:doi.org/10.1002/anie.201506085
14) “Catalysis by electrons and holes: formal potential scales and preparative organic electrochemistry” Luca, R. O.; Gustafson, J. L.; Maddox, S. M.; Fenwick, A. Q.; Smith, D. C, Organic Chemistry Frontiers 2015, 2, 823-848. (doi: https://doi.org/10.1039/C5QO00075K)
13) “A Practical Lewis-Base catalyzed electrophilic chlorination of Arenes and Heterocycles”Maddox, S. M.; Nalbandian, C. J.; Smith, D. E.; Gustafson, J. L. 2015 Organic Letters 17, 1042-1045.
Publications as a Postdoctoral Fellow at Yale University
Publications as a Postdoctoral Fellow at Yale University
12) “HaloPROTACS: Use of Small Molecule PROTACs to Induce Degradation of HaloTag Fusion Proteins.” Buckley, D. L.; Raina, K.; Darricarrerre, N.; Hines, J.; Gustafson, J. L.; Smith, I. E.; Miah, A. H.; Harling, J. D.; Crews, C. M. ACS Chem. Biol. 2015, 10, 1831-1837.
11) “Catalytic in vivo Protein Knockdown by small-molecule PROTACS” Bondeson, D. P.; Mares, A.; Smith, I. E. D.; Ko, E.; Campos, S.; Miah, A. H.; Mulholland, K. E.; Routly, N.; Buckley, D. L.; Gustafson, J. L.; Zinn, N.; Grandi, P.; Shimamura, S.; Bergamini, G.; Faelth-Savitski, M.; Bantscheff, M.; Cox, C.; Gordon, D. A.; Willard, R. R.; Flanagan, J. J.; Casillas, L. N.; Votta, B. J.; den Besten, W.; Famm, K.; Kruidenier, L.; Carter, P. S.; Harling, J. D.; Churcher, I.; Crews, C. M. Nature Chem. Bio. 2015 11, 611-617.
10) “Small Molecule Mediated Degradation of the Androgen Receptor Through Hydrophobic Tagging” Gustafson, J. L.; Neklesa, T. K.; Cox, C. S.; Roth, A. G.; Buckley. S. L.; Tae, H.-Y.; Sundberg, T. B.; McDonnell, D. P.; Morris, J. D.; Crews, C. M.; Angew. Chem. Int. Ed. 2015, 54, 9659-9662.
9) “Small Molecule Inhibitors of the Interaction Between the E3 Ligase VHL and HIF1α” Buckley, D. L.; Gustafson, J. L.; Van Molle, I.; Roth, A. G.; Tae, H.S.; Gareiss, P.C.; Jorgensen, W. L.; Ciulli, A.; Crews, C. M. Angew. Chem. Int. Ed. 2012, 51, 11463-11467.
8) ”Identification of Hydrophobic Tags for the Degradation of Stabilized Proteins.”Tae, H. S.; Sundberg, T.; Neklesa, T. K.; Noblin, D. J.: Gustafson, J. L.; Roth, A. G.; Raina, K.; Crews, C. M. ChemBioChem, 2012, 4, 538-541.
Publications as a Graduate Student at Yale University
Publications as a Graduate Student at Yale University
7) “Synthesis of Atropisomerically Defined, Highly Substituted Biaryl Scaffolds through Catalytic Enantioselective Bromination and Regioselective Cross-Coupling.” Gustafson, J. L.; Lim, D.; Barrett, K.; Miller, S. J. Angew. Chem. Int. Ed. 2011, 50, 5025-5029.
6) “Linear Free Energy Relationship Analysis of a Catalytic Desymmetrization of a Diarylmethane-Bis(phenol).” Gustafson, J. L.; Sigman, M. S.; Miller, S. J. Org. Lett. 2010. 12, 2794-2797.
5) “Dynamic Kinetic Resolution of Biaryl Atropisomers via Peptide-Catalyzed Bromination.” Gustafson, J. L.; Lim, D.; Miller, S. J. Science 2010, 328, 1251-1255. [Highlighted in “Better Route To Hard-To-Get Isomers.” Science and Technology section of Chemical and Engineering News, 21 June 2010-issue, page 32.] [Highlighted in Cozzi, P. G.; Emer, E.; Gualandi, A. “Atropselective Organocatalysis” Angew Chem. Int. Ed. 2011, 50, 3847-3849.]
4) “A Case of Remote Asymmetric Induction in the Peptide-Catalyzed Desymmetrization of a Bis(phenol).” Lewis, C. A.; Gustafson, J. L.; Chiu, A.; Balsells, J.; Pollard, D.; Murry, J.; Reamer, R. A.; Hansen, K. B.; Miller, S. J. J. Am. Chem. Soc. 2008, 130, 16358-16365.
Publications as an Undergraduate Student at San Diego State University
Publications as an Undergraduate Student at San Diego State University
3) “Bifunctional Catalysis of Alkene Isomerization and its Applications.” Grotjahn, D. B.; Larsen, C, R; Erdogan, G; Gustafson, J. L; Sharma, A.; Nair, R. Catal. Org. React. 2009, 123, 379-387.
2) “A Convenient Method for Regeneration of Free Thiol from a tert-Butyl Thioether.” Kragulj, E. J.; Gustafson, J. L.; Grotjahn, D. B. Synlett, 2007, 2851-2854.
1) “Extensive Isomerization of Alkenes using a Bifunctional Catalyst: An Alkene Zipper.” Grotjahn, D. B.; Larsen, C. R.; Gustafson, J. L.; Nair, R.; Sharma, A. J. Am. Chem. Soc. 2007, 129, 9592-9593. [see also “Isomerization at a distance.” Science and Technology Concentrates section of Chemical and Engineering News, 23 July 2007 issue, page 29.]
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