Publications
Microtubule Dynamics Inhibitors
69. Molecular Editing of NSC-666719 Enabling Discovery of benzodithiazinedioxide-guanidines as Anticancer Agents, Vajja Krishna Rao, Subarno Paul, Mitchell Gulkis, Zhihang Shen, Haritha Nair, Amandeep Singh, Chenglong Li, Arun K. Sharma, Melike Çağlayan, Chinmay Das, Biswajit Das, Chanakya N. Kundu, Satya Narayan and Sankar K. Guchhait, RSC Med. Chem. 2024.
68. Molecular medicinal insights into scaffold hopping-based drug discovery success, Ayan Acharya, Mukul Yadav, Mithilesh Nagpure, Sanathanalaxmi Kumaresan, Sankar K. Guchhait, Drug Discov. Today, 2024, 29, 103845.
67. Natural product-inspired discovery of trimethoxyphenyl-1,2,4-triazolo sulfonamides as potent tubulin polymerization inhibitors, Vajja Krishna Rao, Anvesh Ashtam, Dulal Panda, and Sanka K. Guchhait, ChemMedChem 2023, e202300562.
66. Development of QTMP: A promising anticancer agent through NP-Privileged Motif-Driven structural modulation, Pritam Giri, Pooja J. Batra, Ayan Acharya, Anuradha Kumari, Sankar Kumar Guchhait, Neha Hura, Dulal Panda, Bioorg. Med. Chem. 2023, 95, 117489.
65. Scaffold Hopping in Drug Discovery: Innovation in Pharma Industries and Academia, Santhanalaxmi Kumaresan, Jagroop Singh, Ayan Acharya, Mukul Yadav, Sankar K. Guchhait, Current Research & Information on Pharmaceutical Sciences (CRIPS), 2023, 16, 94-99.
64. A cascade reaction of indolyl-migratory isocyanide insertion, scaffold rearrangement and redox-neutral event with isocyanide as a C(sp3)H–N synthon efficiently constructs indolylisoindolinones, Shailendra Sisodiya, Ayan Acharya, Mithilesh Nagpure, Nibedita Roy, Santosh K. Giri, Hare Ram Yadav, Angshuman R. Choudhury and Sankar K. Guchhait, Chem. Commun., 2022, 58, 11827
63. “Core-Linker-Polyamine (CLP)” strategy enabling rapid discovery of antileishmanial aminoalkyl-quinoline-carboxamides that target oxidative stress mechanism, Archana P Shah, Neha Hura, Neerupudi Kishore Babu, Nibedita Roy,Vajja Krishna Rao, Anindita Paul, Pradyot Kumar Roy, Sushma Singh, Sankar Kumar Guchhait, ChemMedChem, 2022, 17, e202200109.
62. Organocatalyzed umpolung addition for synthesis of heterocyclic-fused arylidene-imidazolones as anticancer agents, Gulshan Kumar, Chinmay Das, Ayan Acharya, Subhasmita Bhal, Mayank Joshi, Chanakya Nath Kundu, Angshuman Roy Choudhury, Sankar K Guchhait, Bioorg. Med. Chem., 2022, 67, 116835.
61. “Synthesis of heterocyclic-fused furans and dihydrofurans via a (4+1)-annulation with ylide: Exploration of unique reactivity behavior of α-carbonyl sulfoxonium ylide” Gulshan Kumar, Mithilesh Nagpure, Vajja Krishna Rao, Sankar K. Guchhait, Eur. J. Org. Chem., 2022, e202200193.
60. Identification of 2-arylquinazolines with alkyl-polyamine motifs as potent antileishmanial agents: Synthesis and biological evaluation studies, Anjila Kumari, Tara Jaiswal, Vinay Kumar, Neha Hura, Gulshan Kumar, Neerupudi Kishore Babu, Ayan Acharya, Pradyot K. Roy, Sankar Kumar Guchhait and Sushma Singh, RSC Med. Chem. 2022, 13, 320 - 326.
59. Exploration of Benzo[b]carbazole-6,11-diones as anticancer agents: Synthesis and studies of hTopoIIα inhibition and apoptotic effects, Shailendra Sisodiy, Subarno Paul, Hitesh K. Chaudhary, Preeti Grewal, Gulshan Kumar, Divine P Daniel, Biswajit Das, Deepika Nayak, Sankar K. Guchhait,* Chanakya N. Kundu, Uttam C. Banerjee, Bioorg. Med. Chem. Lett. 2021, 49, 128274.
58. Annulation of conjugated azine-imine with a sulfoxonium ylide in a noncarbenoid route to synthesize multisubstituted imidazole-fused heterocycles, Sankar K. Guchhait, Meenu Saini, Viren J. Khivsara, and Santosh K. Giri, J. Org. Chem. 2021, 86, 5380–5387.
57. Microtubule-targeting agents impair kinesin- 2-dependent nuclear transport of β- catenin: Evidence of inhibition of Wnt/β-catenin signaling as an important antitumor mechanism of microtubule- targeting agents, Anuradha Kumari, Omprakash Shriwas, Shailendra Sisodiya, Manas K. Santra, Sankar K. Guchhait, Rupesh Dash, Dulal Panda, FASEB J. 2021, 35,1-16.
56. Chan-Lam N–arylation and C–H amination with heteroaromatic ring-NH: An approach to access extended-fused imidazo[1,2-a]-pyridines/pyrazines, Sankar K. Guchhait, Meenu Saini, New J. Chem. 2020, 44, 308.
55. C12, a combretastatin-A4 analog, exerts anticancer activity by targeting microtubules; Anuradha Kumari, Shalini Srivastava, Rajesh K. Manne, Shailendra Sisodiya, Manas K. Santra, Sankar K.Guchhait, Dulal Panda, Biochem. Pharmacol. 2019, 170, 113663.
54. C-12 Binds to Tubulin at the Colchicine-binding Site and Target Microtubules by Preferentially Binding to GTP-bound Tubulin, Shweta Shyam Prassanawar, Anuradha Kumari, Sankar K Guchhait, Dulal Panda, FASEB J. 2019, 1, 784.
53. Pharmacoinformatics analysis of merbarone binding site in human topoisomerase IIa, Neha Tripathi, Sankar K. Guchhait, Prasad V. Bharatam, J. Mol. Graph. Model. 2019, 1, 1-18.
52. Combretastatin-Inspired Heterocycles as Antitubulin Anticancer Agents, Neha Hura, Avishkar V. Sawant, Anuradha Kumari, Sankar K. Guchhait, and Dulal Panda, ACS Omega, 2018, 3, 9754−9769.
51. A Combretastatin Analogue C12 Binds to Colchicine Site in Tubulin, Inhibits Spindle Microtubule Dynamics, Activates Mitotic Checkpoint and Induces Apoptosis in Cancer Cells, Anuradha Kumari, Shalini Srivastava, Shweta Shyam Prassanawar, Shailendra Sisodiya, Sankar K.Guchhait, Dulal Panda, Biophys. J. 2018, 114, 415.
50. Synthesis of polyfunctionalized pyrroles via a tandem reaction of Michael addition and intramolecular cyanide-mediated nitrile-to-nitrile condensation, Sankar K. Guchhait, Shailendra Sisodiya, Meenu Saini, Yesha V. Shah, Gulshan Kumar, Divine P Daniel, Neha Hura and Vikas Chaudhary, J. Org. Chem. 2018, 83, 5807–5815.
49. Drug-Clinical Agent Molecular Hybrid: Synthesis of Diaryl(trifluoromethyl)pyrazoles as Tubulin Targeting Anticancer Agents, Neha Hura, Afsana Naaz, Shweta S. Prassanawar, Sankar K. Guchhait, and Dulal Panda; ACS Omega, 2018, 3, 1955−1969.
48. A nitrile-stabilized ammonium ylide as a masked C–C=N synthon in heterocyclization with amidine–imine: 3-component assembly to fused pyrimidine scaffolds, Sankar K. Guchhait, Meenu Saini, Divyani Sumkaria and Vikas Chaudhary, Chem. Commun. 2017, 53, 6941–6944.
47. Synthesis of polysubstituted 2-aminoimidazoles via alkene diamination of guanidine with conjugated α-bromoalkenones, Sankar K. Guchhait, Neha Hura, and Archana P. Shah, J. Org. Chem. 2017, 82, 2745−2752. The article was highlighted for its important insight in Synfacts 2017, 13, 0472.
46. Pyridine C3-arylation of nicotinic acids accessible via a multicomponent reaction: an entry to all substituted-3,4-diarylated pyridines, Sankar K. Guchhait, Neha Hura, Kanchan Sinha and Dulal Panda, RSC Adv., 2017, 7, 8323–8331.
45. Scaffold-Hopping of Aurones: 2-Arylideneimidazo[1,2-a]pyridinones as topoisomerase IIα- inhibiting anticancer agents, Garima Priyadarshani, Anmada Nayak, Suyog M. Amrutkar, Sarita Das, Sankar K. Guchhait, Chanakya N. Kundu, and Uttam C. Banerjee, ACS Med. Chem. Lett. 2016, 7, 1056−1061.
44. Scaffold-hopping of bioactive flavonoids: Discovery of arylpyridopyrimidinones as potent anticancer agents that inhibit catalytic role of topoisomerase IIα, Garima Priyadarshani, Suyog Amrutkar, Anmada Nayak, Uttam C. Banerjee, Chanakya N. Kundu, Sankar K. Guchhait, Eur. J. Med. Chem. 2016, 122, 43-54.
43. Novel combretastatin–2-aminoimidazole analogues as potent tubulin assembly inhibitors: Exploration of unique pharmacophoric impact of bridging skeleton and aryl moiety, Vikas Chaudhary, Jubina Balan Venghateri, Hemendra Pal Singh Dhaked, Anil Shamraj Bhoyar, Sankar K Guchhait, Dulal Panda, J. Med. Chem. 2016, 59, 3439−3451.
42. Oxidative dearomatization of indoles via Pd-catalyzed C–H oxygenation: An entry to C2- quaternary indolin-3-ones; Sankar K. Guchhait, Vikas Chaudhary, Vijay A. Rana, Garima Priyadarshani, Somnath Kandekar, Maneesh Kashyap, Org. Lett. 2016, 18, 1534-1537.
41. Identification of leads for antiproliferative activity on MDA-MB-435 human breast cancer cells through pharmacophore and CYP1A1-mediated metabolism, Prajwal P Nandekar, Kailas Khomane, Vikas Chaudhary, Vijay P Rathod, Roshan M Borkar, Murali Mohan Bhandi, R Srinivas, Abhay T Sangamwar, Sankar K Guchhait, Arvind K Bansal, Eur. J. Med. Chem. 2016, 115, 82-93.
40. A reaction of 1,2-diamines and aldehydes with silyl cyanide as cyanide pronucleophile to access 2-aminopyrazines and 2-aminoquinoxalines, Sankar K. Guchhait, Garima Priyadarshani and Nikhil M. Gulghane, RSC Adv. 2016, 6, 56056–56063.
39. Pd-Catalyzed Ag(I)-promoted C3-arylation of pyrido[1,2‐a]pyrimidin-4-ones with bromo/iodo- arenes, Guchhait, S. K.; Priyadarshani, G.; J. Org. Chem. 2015, 80, 8482−8488.
38. Synthesis of 2-arylpyridopyrimidinones, 6-aryluracils and tri- and tetra-substituted conjugated alkenes via Pd-catalyzed enolic C–O bond activation-arylation, Guchhait, S. K.; Priyadarshani, G.; J. Org. Chem. 2015, 80, 6342−6349.
37. Switch in site of inhibition: a strategy for structure-based discovery of human topoisomerase IIα catalytic inhibitors, Baviskar, A. T.; Amrutkar, S. M.; Trivedi, N.; Chaudhary, V.; Nayak, A.; Guchhait, S. K.; Banerjee, U. C.; Bharatam, P.V.; Kundu, C. N. ACS Med. Chem. Lett., 2015, 6, 481-485.
(This article was considered by the Editor, as an excellent piece of research work and was highlighted by featuring it as cover art image in one of the issues (April, 2015) of the ACS Med.Chem. Lett.)
36. Scaffold-hopping and hybridization based design and building block strategic synthesis of pyridine-annulated purines: discovery of novel apoptotic anticancer agents, Chaudhary, V.; Das, S.; Guchhait, S. K.; Kundu, C. RSC Adv. 2015, 5, 26051-26060.
35. Desilylative activation of TMSCN in chemoselective Strecker–Ugi type reaction: functional fused imidazoles as building blocks as an entry route to annulated purines, Guchhait, S. K.; Chaudhary, V. Org. Biomol. Chem. 2014, 12, 6694-6705. (Cited in ChemInform, 2015, 46, DOI:10.1002/chin.20150603)
34. α,β-Epoxy Esters in Multiple C–O/C–N Bond-Breaking/Formation with 2-Aminopyridines; Synthesis of Biologically Relevant (Z)-2-Methylene-imidazo[1,2-a]pyridin-3-ones, Guchhait, S. K.; Priyadarshani, G.; Hura, N. Synlett. 2014, 25, 1692-1696.
33. Combretastatin A-4 Inspired Novel 2-Aryl-3-arylamino-imidazopyridines/pyrazines as Tubulin Polymerization Inhibitors, Antimitotic and Anticancer Agents, Sanghai, N.; Jain, V.; Preet, R.; Kandekar, S.; Das, S.; Trivedi, N.; Mohapatra, P.; Priyadarshani, G.; Kashyap, M.; Das, D.; Sathapathy, S, R.; Sidharth, S.; Guchhait, S. K.; Kundu. C.; Bharatam, P. V. Med. Chem. Commun. 2014, 5, 766-782.
32. One-pot preparation of isocyanides from amines and their multicomponent reactions: crucial role of dehydrating agent and base, Guchhait, S. K.; Priyadarshani, G.; Chaudhary, V.; Seladiya, S. R.; Shah, T. M.; Bhogayta, N. P. RSC Adv. 2013, 3, 10867–10874.
31. "Structural Elaboration of a Natural Product: Identification of 3, 3′‐Diindolylmethane Aminophosphonate and Urea Derivatives as Potent Anticancer Agents, Kandekar, S.; Preet, R.; Kashyap, M.; Kashyap, M.; Prasad, R.; Mohapatra, P.; Das, D.; Satapathy, S. R.; Sidharth, S.; Jain, V.; Choudhari, M.; Kundu, C. N.; Guchhait, S. K.; Bharatam, P. V. Chem.Med.Chem. 2013, 11, 1873-1884.
30. Indenoindolone derivatives as topoisomerase II–inhibiting anticancer agents, Kashyap, M.; Kandekar, S.; Baviskar, A. T.; Das, D.; Preet, R. Mohapatra, P.; Satapathy, S. R.; Siddharth, S.; Guchhait, S. K.; Kundu, C. N.; Banerjee, U. C. Bioorg. Med. Chem. Lett. 2013, 23, 934-938.
29. C−H Bond Functionalization Under Metalation−Deprotonation Process: Regioselective Direct Arylation of 3‐Aminoimidazo[1,2-a]pyrazine. Guchhait, S. K.; Kandekar, S.; Kashyap, M.; Taxak, N.; Bharatam, P. V. J. Org. Chem. 2012, 77, 8321-8328.
28. A chemoselective Ugi-type reaction in water using TMSCN as a functional isonitrile equivalent: generation of heteroaromatic molecular diversity, Guchhait, S. K.; Chaudhary, V.; Madaan, C. Org. Biomol. Chem. 2012, 10, 9271-9277. (Cited in ChemInform, 2013, 44, DOI: 10.1002/chin.201318035)
27. One-Pot Three-Step Cu-Catalyzed Five/Four-Component Reaction Constructs Polysubstituted Oxa/Thia-zolidin-2-imines, Madaan, C.; Saraf, S.; Priyadarshani, G.; Reddy, P. P.; Guchhait, S. K.; Kunwar, A. C.; Sridhar, B. Synlett. 2012, 23, 1955-1959.
26. Intramolecular oxidative coupling of 3-indolylarylketones with Pd(II)-catalysis under air: convenient access to indenoindolones, Guchhait, S. K.; Kashyap. M.; Kandekar, S. Tetrahedron Lett. 2012, 53, 3919.
25. CuSO4–Glucose for In Situ Generation of Controlled Cu(I)-Cu(II) Bi-catalysts: Multicomponent Reaction of Heterocyclic Azine and Aldehyde with Alkyne, and Cycloisomerization Towards Synthesis of N-Fused Imidazoles, Guchhait, S. K.; Chandgude, A. L.; Priyadarshani, G. J. Org. Chem. 2012, 77, 4438.
(The work was highlighted in an organic chemistry portal, http://www.organic- chemistry.org/abstracts/lit3/627.shtm)
24. Scaffold hybridization in generation of indenoindolones as anticancer agents that induce apoptosis with cell cycle arrest at G2/M phase, Kashyap, M.; Das, D.; Preet, R.; Mohapatra, P.; Satapathy, S. R.; Siddharth, S.; Kundu, C. N., Guchhait, S. K. Bioorg. Med. Chem. Lett. 2012, 22, 2474.
23. Friedel–Crafts 3-(2-bromo)benzoylation of indoles and intramolecular direct arylation: An efficient route to indenoindolones, Guchhait, S. K.; Kashyap, M. Synthesis, 2012, 619.
22. N-Fused imidazoles as novel anticancer agents that inhibit catalytic activity of topoisomerase IIα and induce apoptosis in G1/S phase. Baviskar, A. T.; Madaan, C.; Ranjan Preet; Mohapatra, P.; Jain, V.; Agarwal, A. Guchhait, S. K.; Kundu, C. N.; Banerjee, U. C.; Bharatam, P. V. J. Med. Chem. 2011, 54, 5013-5030. The article was recognized as “highly cited article”; The American Chemical Society appreciated with a certificate.
21. ZrCl4–Mediated regio- and chemoselective Friedel-Crafts acylation of Indole. Guchhait, S. K.; Kashyap, M.; Kamble, H. J. Org. Chem. 2011, 76, 4753-4758.
20. Groebke-Blackburn-Bienaymé multicomponent reaction in scaffold modification of adenine, guanine, and cytosine: Synthesis of aminoimidazole-condensed nucleobases. Guchhait, S. K.; Madaan, C. Tetrahedron Lett. 2011, 52, 56-58.
19. Towards molecular diversity: dealkylation of tert-butyl amine in Ugi-type multicomponent reaction product establishes tert-butyl isocyanide as a useful convertible isonitrile. Guchhait, S. K.; Madaan, C. Org. Biomol. Chem. 2010, 3631-3634.
18. Direct C-H bond arylation of (hetero)arenes with aryl and heteroarylboronic acids. Guchhait, S. K.; Kashyap, M.; Saraf, S. Synthesis, 2010, 1166.
17. A new process of multicomponent Povarov reaction-aerobic dehydrogenation: Synthesis of polysubstituted quinolines. Guchhait, S. K.; Madaan, C.; Jadeja, K. Tetrahedron Lett. 2009, 50, 6861-6865.
16. A highly flexible and efficient Ugi-type multicomponent synthesis of versatile N-fused aminoimidazoles. Guchhait, S. K.; Madaan, C.; Thakkar, B. S. Synthesis, 2009, 3293-3300.
15. An efficient regioselective versatile synthesis of N-fused 2- and 3-aminoimidazoles via Ugi-type multicomponent reaction mediated by zirconium(IV) chloride in polyethylene glycol-400. Guchhait, S. K.; Madaan, C. Synlett, 2009, 628.
14. Synthesis and structure-activity relationships of metal-ligand complexes that potently inhibit cell migration. Beshir, A. B., Guchhait, S. K., José, A. G.; Fenteany, G. Bioorg. Med. Chem. Lett. 2008, 18, 498.
13. Convenient synthesis of α,β-unsaturated phosphonates via a Mizoroki-Heck reaction of arylboronic acids with diethyl vinylphosphonate. Kabalka, G. W.; Guchhait, S. K.; Naravane, A. Tetrahedron Lett. 2004, 45, 4685.
12. Convenient synthesis of α,β-unsaturated sulfones via a Mizoroki-Heck reaction of arylboronic acids with phenyl vinyl sulfones. Kabalka, G. W.; Guchhait, S. K. Tetrahedron Lett. 2004, 45, 4021.
11. Synthesis of diprotected monosubstituted hydrazine derivatives from tert-butyl carbazates and boronic acids. Kabalka, G. W.; Guchhait, S. K. Org. Lett. 2003, 5, 4129.
10. Synthesis of (E)- and (Z)-alkenylphosphonates using vinylboronates. Kabalka, G. W.; Guchhait, S. K. Org. Lett. 2003, 5, 729.
9. Zinc tetrafluoroborate–catalyzed Mannich-type reaction of aldimines and silyl enol ethers in aqueous medium. Ranu, B. C.; Samanta, S.; Guchhait, S. K. Tetrahedron, 2002, 58, 983.
8. Selective reduction of terminal alkynes to alkenes by indium metal. Ranu, B. C.; Dutta, J.; Guchhait, S. K. J. Org. Chem. 2001, 66, 5624.
7. Indium metal as a reducing agent. Selective reduction of carbon-carbon double bond in highly activated conjugated alkenes. Ranu, B. C.; Dutta, J.; Guchhait, S. K. Org. Lett. 2001, 3, 2603.
6. Stereoselective reduction of aryl-substituted gem-dibromides to vinyl bromides by indium metal. Ranu, B. C.; Samanta, S.; Guchhait, S. K. J. Org. Chem. 2001, 66, 4102.
5. Construction of bicyclo[2.2.2]octanone systems by microwave-assisted solid phase Michael addition followed by Al2O3-mediated intramolecular aldolisation. An eco-friendly approach. Ranu, B. C.; Guchhait, S. K.; Ghosh; K.; Patra, A. Green Chem. 2000, 5.
4. A convenient and efficient procedure for selective deprotection of acetates by titanium(IV) isopropoxides. Ranu, B. C.; Guchhait, S. K.; Saha, M. J. Indian Chem. Soc. 1999, 76, 547. (Special issue dedicated to Professor D. Nasipuri, India on the occasion of his 75th birth anniversary)
3. Catalytic hydrogen transfer reductions using ammonium formate. A review. Ranu, B. C.; Sarkar, A.; Guchhait; S. K.; Ghosh, K. J. Indian Chem. Soc. 1998, 75, 690-694. (Special issue dedicated to Professor Sukh Dev, India on the occasion of his 75th birthday)
2. Stereoselective debromination of aryl-substituted vic-dibromide with indium metal. Ranu, B. C.; Guchhait, S. K.; Sarkar, A. Chem. Commun. 1998, 19, 2113-2114.
1. Chemoselective hydrogenation of , -unsaturated sulfones and phosphonates via palladium- assisted hydrogen transfer by ammonium formate. Ranu, B. C.; Guchhait, S. K.; Ghosh, K. J. Org. Chem. 1998, 63, 5250.
Book Chapters
1. “Late Stage C–H Activation-Functionalization of Drugs, Natural Products, and Biomolecules: In View of Molecular Property and Mechanistic Pathway”, Sankar K. Guchhait, Vajja Krishna Rao, Acharya Ayan; a chapter in the book entitled “Handbook of C-H Functionalization (CHF)”, edited by Debabrata Maiti, IIT, Bombay, John Wiley & Sons, Ltd, Chichester, UK, 2021.
2. “Pharmacoinformatics Studies on Human Topoisomerase II: Exploring the Mechanism of Enzyme Inhibition” Chapter 2, pp. 49-142, Neha Tripathi, Rahul Deb, Sankar K. Guchhait and Prasad V. Bharatam*, in the book “Topoisomerase Inhibitors: Classification, Mechanisms of Action and Adverse Effects”, Edited by Raj Kumar and Sandeep Singh, Publishers – Nova Science Publishers, International (USA) publishers, 2017.