Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
Email: lddd@benthamscience.org


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

Author(s): Nitin Kumar, Devender Pathak.

Graphical 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.

Order Reprints Order Eprints Rights & PermissionsPrintExport

Article Details

Year: 2015
Page: [760 - 765]
Pages: 6
DOI: 10.2174/1570180812666150430002118
Price: $58