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Please use this identifier to cite or link to this item: http://repository.iitr.ac.in/handle/123456789/1157
Title: Grinding and Microwave-assisted Synthesis of Heterocyclic Molecules in High Yields and Their Biological Evaluation
Authors: Kumar S.
Kumar A.
Kumar N.
Roy P.
Sondhi S.M.
Published in: Journal of Heterocyclic Chemistry
Abstract: Cis-cyclohexane1,2-dicarboxylic acid (1a), phthalic acid (1b), and pyrazine 2,3- dicarboxylic acid (1c) on grinding with hydrazine hydrate (2a) gave 2-aminohexahydro-1H-isoindole-1,3(2H)-dione (3a), 2-amino-1H-isoindole-1,3(2H)-dione (3b), and 6-amino-5H-pyrrolo[3,4-b]pyrazine-5,7(6H)-dione (3c), respectively. Condensation of (3a, 3b, 3c) with aldehydes (4x, 4y, 4z) and 2-cyanopyridine, 4-cyanopyridine, 2-cyanopyrazine (5x, 5y, 5z) under microwave irradiation gave corresponding azomethine (6ax, 6ay, 6az, 6bx, 6by, 6bz, 6cx, 6cy, 6cz) and amidine (7ax, 7ay, 7az, 7bx, 7by, 7bz, 7cx, 7cy, 7cz) derivatives, respectively. Fully characterized azomethine (6ax, 6ay, 6az, 6bx, 6by, 6bz, 6cx, 6cy, 6cz) and amidine (7ax, 7ay, 7az, 7bx, 7by, 7bz, 7cx, 7cy, 7cz) derivatives were screened for anti-inflammatory and anticancer activity against five human cancer cell lines. Compound 7cx exhibited 35% anti-inflammatory activity at a dose of 50 mg/kg p.o. whereas standard drug ibuprofen showed 39% activity at a dose of 50 mg/kg p.o. Compounds 6bz, 7cx, 7cz (breast T47D), 6bz, 6cy (lung NCI H-522), 6bx, 7bz (colon HCT-15), 6bz (ovary PA-1) and 6bx, and 6cz (liver HepG-2) exhibited good (35–41% inhibition at 10 ?M c) anticancer activity. IC50values of 6bx, 6bz, 6cy, 6cz, 7bz, 7cx, and 7cz against various cancer cell lines and normal cell (COS-1) are also reported. © 2015 HeteroCorporation
Citation: Journal of Heterocyclic Chemistry (2016), 53(6): 1761-1770
URI: https://doi.org/10.1002/jhet.2481
http://repository.iitr.ac.in/handle/123456789/1157
Issue Date: 2016
Publisher: HeteroCorporation
ISSN: 0022152X
Author Scopus IDs: 57216459762
57209569608
57201756182
35509207200
7006090710
Author Affiliations: Kumar, S., Department of Chemistry, Indian Institute of Technology-Roorkee, Roorkee, Uttarakhand 247667, India
Kumar, A., Department of Chemistry, Indian Institute of Technology-Roorkee, Roorkee, Uttarakhand 247667, India
Kumar, N., Department of Biotechnology, Indian Institute of Technology-Roorkee, Roorkee, Uttarakhand 247667, India
Roy, P., Department of Biotechnology, Indian Institute of Technology-Roorkee, Roorkee, Uttarakhand 247667, India
Sondhi, S.M., Department of Chemistry, Indian Institute of Technology-Roorkee, Roorkee, Uttarakhand 247667, India
Corresponding Author: Sondhi, S.M.; Department of Chemistry, Indian Institute of Technology-RoorkeeIndia; email: sondifcy@iitr.ernet.in
Appears in Collections:Journal Publications [BT]

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