Synthesis and antitumor activity of simplified ecteinascidin-saframycin analogs

Synthesis and antitumor activity of simplified ecteinascidin-saframycin analogs
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DOI:
10.1016/j.bmcl.2005.11.069
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发表时间:
2006-03-01
影响因子:
2.7
通讯作者:
Li, HY
Li, HY
中科院分区:
医学4区
文献类型:
--
作者:
Liu, ZZ;Wang, Y;Li, HY

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由左旋多巴制备了海鞘素-红霉素型生物碱的两个系列的简化类似物。针对三种人类癌细胞系(HCT-8 结肠癌、Bel-7402 肝癌和 BGC-823 胃癌)测试了它们的体外抗肿瘤活性。在这些化合物中,酯类似物通常比酰胺类似物具有更强的活性。其中1-萘甲酸酯类似物31针对BGC-823细胞的活性最强。 F (C) 2005 Elsevier Ltd. 保留所有权利。
Two series of simplified analogs of the ecteinascidin-saframycin type alkaloids were prepared from L-DOPA. Their in vitro antitumor activity was tested against three human cancer cell lines (HCT-8 colon carcinoma, Bel-7402 liver carcinoma, and BGC-823 gastric carcinoma). Among these compounds, the ester analogs have stronger activities than those of amide analogs in general. Among them, 1-naphthalene carboxylate ester analog 31 has the strongest activity against BGC-823 cells. F (C) 2005 Elsevier Ltd. All rights reserved.