Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 55, Issue -, Pages 455-461Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2012.06.057
Keywords
Click chemistry; Isatin conjugates; 1H-1,2,3-Triazole; Anticancer evaluation; Structure-activity relationship
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1H-1,2,3-triazole tethered isatin conjugates have been synthesized and evaluated for cytotoxicity on four human cancer cell lines. The results revealed 5a, 5c, 5e and 5n proved to be twice as potent as 5-fluorouracil on THP-1 cell line with Sa and 5c being most active exhibiting IC50 values of <1 against all cell lines except Caco-2. Activity profiles showed dependence on the substituents on isatin rings with a preference for hydrogen while a strong electron withdrawing fluoro as well as nitro substituents on either ring decreased the anticancer activity. (C) 2012 Elsevier Masson SAS. All rights reserved.
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