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KMID : 1059520090530010034
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Journal of the Korean Chemical Society
2009 Volume.53 No. 1 p.34 ~ p.41
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Synthesis of Hydrazone Derivatives of 4-(2-Chloroethyl) semicarbazide : A New Class of Cytotoxic Agents
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El-Sabbagh O. I.
El-Sadek M. E.
Aboukull M. E.
Shallal H. M.
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Abstract
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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 (IC50 = 6 and 8 μg/ml, respectively). Among the 3-formylindole derivatives, 4a (hydrazone of 3-formylindole itself) showed a pronounced cytotoxic activity against both U251 (IC50 = 21 μg/ml) and Hepg2 (IC50 = 7 μg/ml).
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KEYWORD
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Hydrazones, 2-(Chloroethyl)ureas, 4-(2-Chloroethyl) semicarbazides, Cytotoxic activity
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