Abstract
In this paper some semicarbazide and 1,2,4-triazolin-5-one derivatives are evaluated in vitro for their anticancer activity towards human tumour cell line: ovary (TOV 112D), lung (A 549), breast (T47D) and uterus (Hela). Compounds 2-4 have been found to show the most effective in vitro activity against ovary cancer cell line. For compound 4 the growth inhibition (80% and 70%) is observed in two concentrations (100 μg/ml and 50 μg/ml). The cytotoxic effect of examined compounds seems to be dose-dependent and time-dependent. Compound 7 has GI=80% values towards the breast cancer cell line in concentration of 100 μg/ml. Structure-activity relationship (SAR) studies are carried out for all the compounds of the series. Compounds 2-4 show an activity profile that can be improved through medicinal chemistry strategies.
Keywords: Anticancer activity, Cytotoxicity, Isocyanate, Semicarbazide, Synthesis, 1, 2, 4-Triazol-5-one
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