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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Design, Synthesis and Evaluation of Novel 9-substituted Carbazole Derivatives as Potential Anticancer Agents

Author(s): Nitin Kumar and Devender Pathak

Volume 12 , Issue 9 , 2015

Page: [760 - 765] Pages: 6

DOI: 10.2174/1570180812666150430002118

Price: $65

Abstract

The inhibition property of numerous carbazole derivatives for topoisomerase enzyme was checked by molecular docking which were designed by ChemDraw software followed by 3D optimization. Two series i.e. 2-[(4, 5-dihydro-2-substitutedphenyl)imidazol-1-ylamino]-1-(9H-carbazol-9-yl)ethanone (3a-3e) and 2-(9H-carbazol-9-yl)-N'-{[(4-substitutedphenyl) (piperazin-1-yl)]methyl}acetohydrazide (6a-6e) were found to be potent with minimum binding energy. Above mentioned compounds were synthesized by starting with carbazole and characterized by FTIR, 1H-NMR, 13C-NMR, MASS spectrometry and elemental analysis. All the synthesized compounds were evaluated for their anticancer activity by SRB assay method against Human Breast Cancer Line (MCF7). All the tested compounds showed moderate to good anticancer activity. Compound 3d and 6c exhibited highest activity toward the inhibition of cancer cell line.

Keywords: Anticancer activity, carbazole, human breast cancer cell line, sulphorhodamine b assay, topoisomerase-I.

Graphical Abstract

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