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

Journal of the Korean Chemical Society

M E Aboukull¹  M E El Sadek¹  O I El Sabbagh¹  H M Shallal¹ 

关键词: Hydrazones;    2-(Chloroethyl)ureas;    4-(2-Chloroethyl) semicarbazides;    Cytotoxic activity;   

DOI  :  

学科分类：化学（综合）

来源: Korean Chemical Society

【 摘 要 】

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 ¥ìg/ml, respectively). Among the 3-formylindole derivatives, 4a (hydrazone of 3-formylindole itself) showed a pronounced cytotoxic activity against both U251 (IC50 = 21 ¥ìg/ml) and Hepg2 (IC50 = 7 ¥ìg/ml).

【 授权许可】

Unknown