Thiophene-3-carboxamide analogue of annonaceous acetogenins as antitumor drug lead
Thiophene-3-carboxamide analogue of annonaceous acetogenins as antitumor drug lead
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DOI：
10.1016/j.ejmech.2014.09.026
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发表时间：
2014-10-30
影响因子：
6.7
通讯作者：
Yamashita, Masayuki
中科院分区：
文献类型：
--
作者：
Kojima, Naoto;Fushimi, Tetsuya;Yamashita, Masayuki
合成了五种新型的含呋喃、噻吩或噻唑环的丙酮配基类似物，并评价了它们对人癌细胞系的抑制活性。这些化合物的活性均高于天然产物。其中之一，噻吩-3-甲酰胺类似物，在异种移植小鼠试验中强烈抑制人肺癌细胞系NCI-H23的生长，而没有临界毒性。(C)2014年Elsevier Masson SAS。All rights reserved.
Five novel acetogenin analogues with a furan, thiophene, or thiazole ring were synthesized, and their inhibitory activities toward human cancer cell lines were evaluated. The analogues showed more potent activities than natural acetogenin. One of them, the thiophene-3-carboxamide analogue, strongly inhibited the growth of human lung cancer cell line NCI-H23 in the xenograft mouse assay without critical toxicity. (C) 2014 Elsevier Masson SAS. All rights reserved.