Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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Anticancer Screening and Structure Activity Relationship Study of Some Semicarbazides and 1,2,4-Triazolin-5-ones

Author(s): Monika Pitucha, Jolanta Rzymowska.

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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Article Details

VOLUME: 9
ISSUE: 6
Year: 2012
Page: [568 - 572]
Pages: 5
DOI: 10.2174/157018012800673047
Price: $58