Synthesis and cytostatic evaluation of some 2-(5-substituted-2-oxoindolin-3-ylidene)-N-substituted hydrazine carbothioamide

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...

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Bibliographic Details
Published in:Medicinal chemistry research 2011-11, Vol.20 (8), p.1229-1234
Main Authors: Karki, Subhas S., Kulkarni, Amol, Teraiya, Nishith, De Clercq, Erik, Balzarini, Jan
Format: Article
Language:English
Subjects:
Biochemistry
Biomedical and Life Sciences
Biomedicine
Cell Biology
Hydrazine
Hydrazines
Leukemia
Lymphocytes
Lymphocytes T
Melphalan
Original Research
Pharmacology/Toxicology
Substitutes
Tumor cells
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Summary: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 (IC 50 ) 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.
ISSN:1054-2523
1554-8120
DOI:10.1007/s00044-010-9458-3