摘要/Abstract

以2-噻吩乙胺与自制的查尔酮酸进行酰化反应得到酰胺类中间体5a~5j, 经Bischer-Napieralski环合反应合成了10个未见报道的二氢噻吩并吡啶-查尔酮衍生物6a~6j, 再经去氢反应获得2个噻吩并吡啶-查尔酮衍生物7a和7b. 通过噻唑蓝(MTT)法对11种细胞进行体外抗癌活性及安全性测试. 结果表明, 化合物6a (p-F)、6d (o-Br)和6h (m-OCH₃)对HeLa、SGC-7901细胞的抗癌活性优于紫杉醇. 当短时间处理(<4 h)时, 6j (3,4,5-OCH₃)在不影响正常细胞MCF-10A的情况下对癌细胞MCF-7显示强效抗癌效果, 值得进一步研究和开发.
关键词: 二氢噻吩并吡啶-查尔酮衍生物, 抗癌活性, 选择性, 药物摄取能力
The amide intermediates 5a~5j were prepared by acylation, which used 2-thiopheneethylamine and several self-synthetic chalcone acids as starting materials. Then ten dihydrothiophenopyridine-chalcone derivatives 6a~6j which haven't been reported before were synthesized by Bischer-Napieralski cyclization reaction from the intermediates. In addition, two new thiophenopyridine-chalconone derivatives 7a and 7b were obtained by further dehydrogenation. The anti-cancer activity and safety in vitro of 11 kinds of cells were evaluated by methyl thiazolyl tetrazolium (MTT) assay. The results indicated that the compounds 6a (p-F), 6d (o-Br) and 6h (m-OCH₃) exerted better anticancer activity against HeLa and SGC-7901 cells than taxol. When treating cells for a short time (<4 h), 6j (3,4,5-(OCH₃)₃) showed strong anticancer activity against MCF-7 cancer cell but displayed little toxicity on normal breast cell MCF-10A. Hence, 6j deserves further research and exploitation.
Key words: dihydrothiophenopyridine-chalcone derivatives, anticancer activity, selectivity, drug uptake capacity


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