Syntheses and antitumor activity of cis-restricted combretastatins: 5-membered heterocyclic analogues

Syntheses and antitumor activity of cis-restricted combretastatins: 5-membered heterocyclic analogues
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DOI:
10.1016/s0960-894x(98)00579-4
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发表时间:
1998-11-17
影响因子:
2.7
通讯作者:
Tsuji, T
Tsuji, T
中科院分区:
医学4区
文献类型:
--
作者:
Ohsumi, K;Hatanaka, T;Tsuji, T

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合成了一系列顺式限制性的5元杂环combretastatin类似物,并评价了它们对微管组装的抑制活性和对结肠26腺癌细胞系的细胞毒活性。一些杂环类似物显示出有效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。(C)1998爱思唯尔科技有限公司版权所有。
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. (C) 1998 Elsevier Science Ltd. All rights reserved.