Synthesis and anticancer evaluation of thiazolyl–chalcones
作者： Hai-Bo Shi , Shi-Jie Zhang , Qiu-Fu Ge , Dian-Wu Guo , Chao-Ming Cai
DOI: 10.1016/J.BMCL.2010.09.041
关键词:
摘要: Thirty-seven (E)-1-(4-methyl-2-arylaminothiazol-5-yl)-3-arylprop-2-en-1-ones were synthesized via Claisen-Schmidt condensation of 1-(4-methyl-2-(arylamino)thiazol-5-yl)ethanone with the corresponding arylaldehydes. All these thiazolyl-chalcones characterized and evaluated by MTT assay on human cancer cell lines BGC-823, PC-3, NCI-H460, BEL-7402 in vitro. Compounds 5, 8, 26, 37 41 are effective against IC(50)s below 10 μM. The antitumor activity ICR mice bearing sarcoma 180 tumors indicates compounds have moderate vivo 22-25% tumor-weight inhibition.
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