Synthesis and evaluation of the biological activity of N′-[2-oxo-1,2 dihydro-3H-indol-3-ylidene] benzohydrazides as potential anticancer agents
Author(s) -
Arpit Katiyar,
Mahesh Hegde,
Sujeet Kumar,
Vidya Gopalakrishnan,
Khyati Bhatelia,
Kavya Ananthaswamy,
Sureshbabu A. Ramareddy,
Erik De Clercq,
Bibha Choudhary,
Dominique Schols,
Sathees C. Raghavan,
Subhas S. Karki
Publication year - 2015
Publication title -
rsc advances
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.746
H-Index - 148
ISSN - 2046-2069
DOI - 10.1039/c5ra01528f
Subject(s) - chemistry , combinatorial chemistry , stereochemistry , medicinal chemistry
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]ben zohydrazide 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
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