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Current Area of Research
Atom-economic and cost-effective synthesis of Sunitinib, Nintedanib, Olaparib
Common people having median income cannot afford the treatment arising from using block buster anticancer drugs. The cost effective non-infringing synthetic routes are targeted for (Sunitinib, Nintedanib and Olaparib) since they are having very high selling price with big sale but possess low number of Drug Master File (DMF) and suppliers in India. Moreover, can we find out an alternative cost effective and non-infringing synthetic routes for Centchroman for its reposition as anticancer agents? Discovered Cost Effective New Process Routes of Olaparib and Nintedanib. (Green Chem., 2023, 25, 9097 ; Organic Process Research & Development 2024, 28, 3, 754-769; Open for Licensing)
Repurposing of Selected Ongoing Clinical Trial Drugs but nonavailable in India as COVID-19 Therapeutics
In absence of suitable therapeutics for COVID-19, we are working to reposition few known off-patent molecules that are not available in India as possible treatment for SARS-CoV2 in collaboration with company, Ahmedabad through innovation of novel synthetic routes and filing patents on them. Research Work has been shared with Reliance Rasayan Private Limited, Ahmedabad
Inhibitors targeting NAD+ binding sites by occupying nicotinamide pocket of Poly ADP Ribose polymerase (PARP)
Olaparib and Rucaparib analogs
Amino Acid based Poly(ADP-ribose)polymerase (PARP) Inhibitors and their application against BRCA mutated cancers (0229NF2023; IN 202411019816)
Chiral Amino acids as well as symmetrical diamino triazine substituted phthalazinones inhibited the growth and development of BRCA2 mutant cells with an IC50 value of the most active compounds in the range of 2-57 nM. The active compounds selectively induce cytotoxicity in BRCA2 mutant cancer cells compared to wild type cells with a mutant fold selectivity in range of 112-419-fold. Most importantly, the active compounds are capable of killing the BRCA mutated cancerous cells and show statistically significant PARP activity as well as show low cytotoxicity to wild type cells
2-Pyridone based quinazoline compounds as dual EZH2 and EGFR Inhibitors (0082NF2024/IN; CDRI; 09-May-2024; IN 202411036881)
2-Pyridone-based quinazoline compound a dual EZH2 and EGFR Inhibitor show better cytotoxic activity in TNBC cells as compared to the individual comparator drug (Tazemetostat-EZH2 inhibitor, Gefitinib- EGFR inhibitor).
Purine Based Phthalazinones as dual PARP and mTOR Inhibitors (0083NF2024/IN; CDRI; 15-May-2024, IN 202411038350)
Purine-based phthalazinones show marked inhibitory activity against both the targets mTOR and PARP and display potent cytotoxic activity not only against BRCA deficient cancer cells like classical PARP inhibitors but also demonstrate their efficacy against BRCA proficient cancer cells.
Pyridine based scaffolds as dual acting Bcl2 and HDAC for autophagy
HDAC inhibitors induced apoptosis and down regulated the expression and over expression of the B-cell lymphomas 2 (Bcl2). Goal is to find pyridine-based scaffolds as double acting role on Bcl2 and HDAC to induce autophagy inside the cancerous cell.
Asymmetric Synthesis of Trisubstituted Methanes (TRSMs) as new bioactives
Our lead TRSM CDRI-830 showed 15-20 fold reduction in the CFU of infected mouse lungs, which was comparable with the efficacy of ethambutol and pyrazinamide. One of the enantiomer S-TRSM (E2) has shown significantly higher MIC and MBC (in vitro as well as ex vivo) than R-TRSM (E1). The goal is to find out new asymmetric cost effective synthesis of individual enantiomers of TRSM for further bioevaluation
Buckybowl Corannulene derived Amphipathic peptides; Synthesis and Studies on synergistic activities
To achieve cationic water-soluble amphipathic peptides derived from corannulene to counter ever emerging multi-drug resistance in bacterial infection. (J. Med. Chem. XXXX, XXX, XXX−XXX in press)
Bucky-Bowl Derived Hydrogelators with Bifunctional chelating agents for removal of Toxic materials and Drug Delivery
Peptide based bowl derived architectures with chelation to remove Toxic substances and for Drug Delivery
Q203-Bedaquiline Hybrids as energy metabolism inhibitors for M Tb
Bedaquiline inhibits M TB ATP synthesis in mycobacteria. Q203 is also acting against MDR and XDR strains of M. tuberculosis. Our target is to synthesize hybrid molecules of bedaquiline and Q203 for potent Anti-Tubercular activity with acceptable side effects.
Selected list of publications
Stereoselective Construction of 3-(aminoalkylidene)Oxindoles in One-Pot: Development of a Novel, Robust and Scalable Process for the Multigram-Scale Preparation of Nintedanib; Saroj Maji, Sabyasachi Halder, Ashok Kumar Sharma, Avinash Madhesiya, Tejender S. Thakur, Gautam Panda*, Organic Process Research & Development 2024, 28, 3, 754-769
Corannulene Amino Acid Derived Water Soluble Amphiphilic Buckybowl as Broad-spectrum Membrane Targeting Antibacterial Agents; Saroj Maji, Sariyah Akhtar, Sabyasachi Halder, Indranil Chatterjee, Devesh Pratap Verma, Neeraj Kumar Verma, Jyotshana Saroj, Deepanshi Saxena, Rahul Maitra, Juhi Sharma, Bhawana Sharma, Hidehiro Sakurai, Kalyan Mitra, Sidharth Chopra, Jimut Kanti Ghosh, Gautam Panda, J. Med. Chem. XXXX, XXX, XXX−XXX
An Efficient Approach Towards the Synthesis of Nintedanib; Saroj Maji, Souvik Barman, Gautam Panda*, ChemistrySelect 2023, 8, e20230096; https://doi.org/10.1002/slct.202300968
A Scalable and Eco-friendly Total Synthesis of Poly (ADP-Ribose) Polymerase Inhibitor Olaparib; Indranil Chatterjee, Deblina Roy and Gautam Panda*, Green Chem., 2023, 25, 9097
A Tandem Semipinacol Rearrangement/aldehyde Arylation or Alkylation of Trisubstituted 2,3-Epoxy Alcohols with Grignard reagents for Functionalized 1,3-diols; Amit Kumar, Gaurav Sharma, Sanjeev K Shukla, Gautam Panda*, Journal of Organic Chemistry 2022, 87, 12, 7696-7711
Tyrosine-Derived Novel Benzoxazine Active in Rat Syngenic Mammary Tumor Model of Breast Cancer, J. Med. Chem. 2021, 64, 16293−16316, doi- 10.1021/acs.jmedchem.1c01624.
Design, Synthesis and Biological evaluation of (Quinazoline 4-yloxy)acetamide and (4-oxoquinazoline-3(4H)-yl)acetamide derivatives as inhibitors of Mycobacterium tuberculosis bd oxidase; Amit Kumar, Neetu Kumari, Sandeep Bhattacherjee, Umamageswaran Venugopal, Shahid Parwez, Mohammad Imran Siddiqi, Manju Y Krishnan and Gautam Panda, Eur J Med Chem accepted; https://doi.org/10.1016/j.ejmech.2022.114639
A Tandem Semipinacol Rearrangement/aldehyde Arylation or Alkylation of Trisubstituted 2,3-Epoxy Alcohols with Grignard reagents for Functionalized 1,3-diols; Amit Kumar, Gaurav Sharma, Sanjeev K Shukla, Gautam Panda, Journal of Organic Chemistry 2022, 87, 12, 7696-7711
Unveiling p-Quinone methide (QM) chemistry to synthesize Bedaquiline (TMC 207) like architectures, Journal of Molecular Structure ,2021, 1239, 130493; https://doi.org/10.1016/j.molstruc.2021.130493
New Spisulosine Derivative Promotes Robust Autophagic Response to Cancer Cells; Eur J Med Chem, 2020, 188, 112011; https://doi.org/10.1016/j.ejmech.2019.112011.
Base mediated 1,6- Aza-Michael addition of heterocyclic amines and amides to p-QMs leading to Meclizine, Hydroxyzine and Cetirizine like architectures, Synthesis 2019, 51, 4434-4442 (10.1055/s-0039-1690677) https://www.thieme.de/en/thieme-chemistry/synform-news-novel-approach-to-antihistamine-type-scaffolds-148429.htm#
Thiophene containing Trisubstituted Methanes [TRSMs] as identified lead against Mycobacterium Tuberculosis; European Journal of Medicinal Chemistry, 2015, 95, 357-368.
Total Synthesis of C3-epi-(+)-Lycoricidine from Garner aldehyde via IntramolecularAldol Cyclization, Tetrahedron Letters, 2015, 56, 146-149
Synthesis of polyhydroxylatedindolizidines and piperidines from Garner's aldehyde: total synthesis of (−)-swainsonine, (+)-1,2-di-epi-swainsonine, (+)-8,8a-di-epi-castanospermine, pentahydroxyindolizidines, (−)-1-deoxynojirimycin, (−)-1-deoxy-altro-nojirimycin, and related diversity, Tetrahedron, 2014, 70, 1363-1374.
Sudipta Kumar Manna and Gautam Panda; Synthesis of enantiomerically enriched indolines and tetrahydroisoquinolines from (S)-amino acidderived chiral carbocations: an easy access to (3S,4R)-demethoxy-3-isopropyl diclofensine, Org. Biomol. Chem, 2014, 11, 8318-24
Stereoselective synthesis of Jaspine B and its C2 epimer from Garner aldehyde
Amit Kumar Jana and Gautam Panda* RSC Adv., 2013, 3, 16795–16801 DOI: 10.1039/ c3ra41778f
Manish Goyal; Priyanka Singh; Athar Alam; Sajal K Das; Mohd S Iqbal; Sumanta Dey; Samik Bindu; Chinmay Pal; Sanjit K Das; Gautam Panda; Uday Bandyopadhyay; Aryl aryl methyl thio arenes prevent multi-drug resistant malaria in mouse by promoting oxidative stress in parasite; Free Radical Biology & Medicine, 2012, 53, 129-42
Application of Nazarov type electrocyclization to access [6-5-6] and [6-5-5] core embedded new Polycycles: an easy entry to tetrahydrofluorene scaffolds related to Taiwaniaquinoids and C-nor-D homosteroids, Org. Biomol. Chem., 2011, 9, 4782-4790 (selected as cover page article).
Samanta, K.; and Panda, G.: Regioselective Ring‐Opening of Amino Acid‐Derived Chiral Aziridines: an Easy Access to cis‐2, 5‐Disubstituted Chiral Piperazines; Chemistry an Asian Journal, 2011, 6, 189-197
Dinda, S. K., Das, S. K., and Panda, G.: Asymmetric total syntheses of spisulosine, its diastereo- and regioisomers, Tetrahedron, 2010, 66, 9304-9309
A convenient synthesis of chiral amino acid derived 3,4-dihydro-2H-benzo[b][1,4]thiazines and antibiotic levofloxacin. Tetrahedron Letters, 2009, 50,4703-4705.
Total Synthesis of (-)-Balanol, its all Stereoisomers, their N-tosyl analogues and fully protected Ophiocordin: An easy access to hexahydroazepine cores from Garner aldehydes. Chemistry A European Journal, 2008, 14, 4675-4688.
Disruptive Innovative Synthetic Attempts for Drugs like Bedaquiline, Dearylated Lasofoxifene, Centchroman, Meclizine and Cetirizine
Target and diversity oriented Synthesis of Bioactive natural products
Extensive, ingenious harnessing of materials towards synthesis of potent bioactive molecules
Quest for Steroidomimetics: Amino Acids Derived Chiral Steroidal and non-steroidal architectures as anti breast cancer agents
In quest for steroidomimetics, employment of chiron Amino Acids to incorporate chiral space towards difficult asymmetric steroids
Syn-2,3-Dihydroxy Esters derived Anticancer molecules
New functionalized synthon to access chiral heterocycles and antimalarial Raphidecursinol B and anticancer Spisulosine
New Spisulosine Derivative Promotes Robust Autophagic Response to Cancer Cells
Subtle changes in chemical structure of spisulosine completely switched its cytotoxic function from apoptosis to autophagy to address therapy resistance, bringing one of the hallmarks of human cancer
Ligand and structure-based screening of designed and synthesized chemical library based on Psammaplin A, Plinabulin, Spisulosine against different kinds of DNA methyltransferase
Chemistry around Chiral Tri and Tetrasubstituted Methanes (TRSMs) as M tb ATP Synthase inhibitors; Asymmetric Synthesis of 9-substituted Xanthenes as constrained TRSMs having anti-TB properties
Thiophene containing trisubstituted methanes [TRSMs] as identified lead against Mycobacterium tuberculosis
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