顺式受限的柯里拉京类似物：五元杂环类似物的合成及其抗肿瘤活性
Syntheses and antitumor activity of cis-restricted combretastatins: 5-membered heterocyclic analogues.
作者信息
Ohsumi K, Hatanaka T, Fujita K, Nakagawa R, Fukuda Y, Nihei Y, Suga Y, Morinaga Y, Akiyama Y, Tsuji T
机构信息
Pharmaceutical Research Laboratories, Ajinomoto Co. Inc., Kawasaki, Japan.
出版信息
Bioorg Med Chem Lett. 1998 Nov 17;8(22):3153-8. doi: 10.1016/s0960-894x(98)00579-4.
A series of cis-restricted combretastatin analogues with 5-membered heterocycles were synthesized and their inhibitory activity against microtubule assembly and cytotoxic activity against the colon 26 adenocarcinoma cancer cell line were evaluated. Some of the heterocyclic analogues showed potent antitubulin activity and cytotoxicity. Compounds 16 and 35 showed marked tumor growth suppression in the colon 26 murine tumor model.
合成了一系列具有五元杂环的顺式受限康普他汀类似物，并评估了它们对微管组装的抑制活性以及对结肠26腺癌癌细胞系的细胞毒性。一些杂环类似物表现出强大的抗微管蛋白活性和细胞毒性。化合物16和35在结肠26小鼠肿瘤模型中显示出显著的肿瘤生长抑制作用。
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