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Please use this identifier to cite or link to this item: http://repository.iitr.ac.in/handle/123456789/1585
Title: Efficient synthesis of piperazine-2,6-dione and 4-(1H-indole-2-carbonyl) piperazine-2,6-dione derivatives and their evaluation for anticancer activity
Authors: Kumar S.
Kumar N.
Roy, Partha
Sondhi S.M.
Published in: Medicinal Chemistry Research
Abstract: Condensation of iminodiacetic acid 1 with various amines i.e., cyclohexanamine, 1-(3-aminopropyl)imidazole, pyridin-2-ylmethanamine, pyridin-3-ylmethanamine, pyridin-4-ylmethanamine, 2-morpholinoethanamine, thiophen-2-ylmethanamine, 2-(thiophen-2-yl)ethanamine, furan-2-ylmethanamine, 2-(pyrrolidin-1-yl)ethanamine, and 1-(3-aminopropyl) pyrrolidin-2-one 2a-k under microwave irradiation gave the corresponding piperazine-2,6-dione derivatives 3a-k in quantitative yields. Piperazine-2,6-dione derivatives 3a-k on condensation with 1H-indole-2-carboxylic acid under microwave irradiation gave the corresponding 4-(1H-indole-2-carbonyl)piperazine-2,6-dione derivatives 4a-k in quantitative yields. All the synthesized compounds (3a-k & 4a-k) were purified by crystallization and characterized by spectroscopic means. On screening at a concentration of 10 ?M, compounds 3k, 4e, 4i breast (T47D), 4j lung (NCI H-522), 3i colon (HCT-15), 4e ovary (PA-1), and 4g liver (HepG-2) exhibited good anticancer activity. © 2013 Springer Science+Business Media New York.
Citation: Medicinal Chemistry Research (2013), 22(10): 4600-4609
URI: https://doi.org/10.1007/s00044-012-0438-7
http://repository.iitr.ac.in/handle/123456789/1585
Issue Date: 2013
Keywords: Anticancer activity
Microwave synthesis
Piperazine dione derivatives
ISSN: 10542523
Author Scopus IDs: 57216459762
57192281884
35509207200
7006090710
Author Affiliations: Kumar, S., Department of Chemistry, Indian Institute of Technology-Roorkee, Roorkee 247667 Uttrakhand, India
Kumar, N., Department of Biotechnology, Indian Institute of Technology-Roorkee, Roorkee 247667 Uttrakhand, India
Roy, P., Department of Biotechnology, Indian Institute of Technology-Roorkee, Roorkee 247667 Uttrakhand, India
Sondhi, S.M., Department of Chemistry, Indian Institute of Technology-Roorkee, Roorkee 247667 Uttrakhand, India
Funding Details: Acknowledgments We are thankful to the technical staff of the Chemistry Department, I. I. T. Roorkee, for spectroscopic studies and elemental analysis and also to Head I. I. C. for providing NMR facility. Special thanks are due to Prof. G. Bhattacharjee and Prof. Ravi Bhushan of Chemistry Department, I. I. T. Roorkee, for helpful discussion. Mr. Sandeep Kumar is thankful to MHRD, New Delhi for financial assistance.
Corresponding Author: Sondhi, S.M.; Department of Chemistry, Indian Institute of Technology-Roorkee, Roorkee 247667 Uttrakhand, India; email: sondifcy@iitr.ernet.in
Appears in Collections:Journal Publications [BT]

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