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http://dx.doi.org/10.5012/jkcs.2009.53.1.034

Synthesis of Hydrazone Derivatives of 4-(2-Chloroethyl) semicarbazide : A New Class of Cytotoxic Agents  

El-Sabbagh, O.I. (Department of Medicinal Chemistry, Faculty of Pharmacy, Zagazig University)
El-Sadek, M.E. (Department of Medicinal Chemistry, Faculty of Pharmacy, Zagazig University)
Aboukull, M.E. (Department of Medicinal Chemistry, Faculty of Pharmacy, Zagazig University)
Shallal, H.M. (Department of Medicinal Chemistry, Faculty of Pharmacy, Zagazig University)
Publication Information
Journal of the Korean Chemical Society / v.53, no.1, 2009 , pp. 34-41 More about this Journal
Abstract
A new series of hydrazone derivatives were synthesized from 4-(2-chloroethyl)semicarbazide and their antiproliferative activity against human brain (U251) and liver (Hepg2) carcinoma cell lines were evaluated. The hydrazone compounds are benzaldehyde (2a-2g), acetophenone (3a-3f), and 3-formylindole derivatives (4a-4d). Among the acetophenone derivatives, 3e (p-methoxy substituted) and 3f (p-nitro substituted) showed the highest cytotoxic activity against Hepg2 cell line (I$C_{50}$ = 6 and 8 $\mu$g/ml, respectively). Among the 3-formylindole derivatives, 4a (hydrazone of 3-formylindole itself) showed a pronounced cytotoxic activity against both U251 (I$C_{50}$ = 21 $\mu$g/ml) and Hepg2 (I$C_{50}$ = 7 $\mu$g/ml).
Keywords
Hydrazones; 2-(Chloroethyl)ureas; 4-(2-Chloroethyl) semicarbazides; Cytotoxic activity;
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