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Issue 56, 2015
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Synthesis and evaluation of the biological activity of N′-[2-oxo-1,2 dihydro-3H-indol-3-ylidene] benzohydrazides as potential anticancer agents

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Abstract

New N′-[2-oxo-1,2-dihydro-3H-indol-3-ylidene]benzohydrazide derivatives were synthesized and evaluated for their cytotoxic properties against murine leukemia, L1210, human leukemia, REH and K562, human T-cell leukemia, CEM and human cervix carcinoma, HeLa cells. Among the tested compounds, the 3,4,5-trimethoxy-N′-[5-methyl-2-oxo-1,2-dihydro-3H-indol-3-ylidene]benzohydrazide derivative (5t) emerged as the most potent inhibitor against all the tumor cell lines evaluated. To investigate the mechanism of action, 5t was further studied by cell cycle analysis, mitochondrial membrane potential analysis, DNA fragmentation and Annexin V-FITC flow cytometric analysis, which suggested that 5t was able to induce apoptosis at submicromolar range.

Graphical abstract: Synthesis and evaluation of the biological activity of N′-[2-oxo-1,2 dihydro-3H-indol-3-ylidene] benzohydrazides as potential anticancer agents

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Supplementary files

Article information


Submitted
29 Jan 2015
Accepted
12 May 2015
First published
13 May 2015

RSC Adv., 2015,5, 45492-45501
Article type
Paper
Author version available

Synthesis and evaluation of the biological activity of N′-[2-oxo-1,2 dihydro-3H-indol-3-ylidene] benzohydrazides as potential anticancer agents

A. Katiyar, M. Hegde, S. Kumar, V. Gopalakrishnan, K. D. Bhatelia, K. Ananthaswamy, S. A. Ramareddy, E. De Clercq, B. Choudhary, D. Schols, S. C. Raghavan and S. S. Karki, RSC Adv., 2015, 5, 45492
DOI: 10.1039/C5RA01528F

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