简化的海鞘素-沙佛霉素类似物的合成及其抗肿瘤活性

Synthesis and antitumor activity of simplified ecteinascidin-saframycin analogs.

作者信息

Liu Zhan-Zhu, Wang Ye, Tang Ye-Feng, Chen Shi-Zhi, Chen Xiao-Guang, Li Hong-Yan

机构信息

Institute of Materia Medica, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing 100050, PR China.

出版信息

Bioorg Med Chem Lett. 2006 Mar 1;16(5):1282-5. doi: 10.1016/j.bmcl.2005.11.069. Epub 2005 Dec 9.

DOI:10.1016/j.bmcl.2005.11.069

PMID:16338237

Abstract

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.

摘要

以L-多巴为原料制备了两类简化的埃博霉素-沙弗霉素型生物碱类似物。测试了它们对三种人类癌细胞系（HCT-8结肠癌、Bel-7402肝癌和BGC-823胃癌）的体外抗肿瘤活性。在这些化合物中，酯类类似物的活性总体上比酰胺类类似物更强。其中，1-萘羧酸酯类似物31对BGC-823细胞的活性最强。