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Synthesis and Cytotoxic Evaluation of some 2-{4-[ (2-Oxo-1,2-Dihydro-3h-Indol-3-Ylidene) methyl] Phenoxy}-N-Phenylacetamide

Bhadauria, V.Singh.; Sravanthi, V.; Kumar, S.; Das, D.; DE Clercq, E.; Schols, D.; Tokuda, H.; Karki, S.S.

Acta Poloniae Pharmaceutica 74(1): 137-145

2017

ISSN/ISBN: 0001-6837
PMID: 29474770
Document Number: 692433
A series of 2-oxindole derivatives were synthesized and evaluated for cytotoxic activity against different human and murine cancer cell lines and cancer chemopreventive activity. Among the tested compounds VS-06, 08, 12 and 17 displayed cytotoxic activity in the range of 5.0 to 8.5 pM against human T-lymphocyte cells (CEM). Results showed that molecules with electron withdrawing substituent at 4 position of N-phenylacetamide group exhibited an increase in activity against the human tumor cell line CEM. The cancer chemo- preventive effect of VS-01 (IC₅₀ = 451 nM) displayed equipotent activity in comparison to standard oleanolic acid (IC₅₀ = 449 nM).

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