Synthesis and cytostatic evaluation of some 2-(5-substituted-2-oxoindolin-3-ylidene)-N-substituted hydrazine carbothioamide |
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Authors: | Subhas S Karki Amol Kulkarni Nishith Teraiya Erik De Clercq and Jan Balzarini |
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Institution: | (1) Department of Pharmaceutical Chemistry, KLE University’s College of Pharmacy, Rajajinagar, Bangalore, 560010, Karnataka, India;(2) Rega Institute for Medical Research, Katholieke Universiteit Leuven, Minderbroedersstraat 10, B-3000 Leuven, Belgium |
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Abstract: | Various substituted 2-(5-substituted-2-oxoindolin-3-ylidene)-N-substituted hydrazine carbothioamide 4a–g and 2-(5-substituted-1-(4-substituted benzyl)-2-oxoindolin-3-ylidene)-N-substituted hydrazine carbothioamide 5a–k were synthesized. The compounds were evaluated for their cytostatic activity against human Molt4/C8 and CEM T-lymphocytes
as well as murine L1210 leukemia cells. Several of these compounds were endowed with low micromolar 50%-inhibitory concentration
(IC50) values, and some were virtually equally potent as melphalan. The most potent inhibitors against the murine leukemia cells
were also most inhibitory against human T-lymphocyte tumor cells. 2-(5-fluoro-1-(4-fluorobenzyl)-2-oxoindolin-3-ylidene)-N-p-tolylhydrazine carbothioamide (5b) emerged as the most potent cytostatic compound among the tested compounds. The encouraging cytostatic data provide an adequate
rationale for further modification of these molecular scaffolds. |
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