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作为潜在抗癌剂的安托芬类似物的合成与构效关系研究。

Synthesis and structure-activity studies of antofine analogues as potential anticancer agents.

作者信息

Fu Ye, Lee Sang Kook, Min Hye-Young, Lee Taeho, Lee Jaekwang, Cheng Maosheng, Kim Sanghee

机构信息

College of Pharmacy, Seoul National University, San 56-1, Shilim, Kwanak, Seoul 151-742, Republic of Korea.

出版信息

Bioorg Med Chem Lett. 2007 Jan 1;17(1):97-100. doi: 10.1016/j.bmcl.2006.09.080. Epub 2006 Sep 30.

DOI:10.1016/j.bmcl.2006.09.080
PMID:17049857
Abstract

Due to the profound cytotoxicities and interesting biochemical aspects, phenanthroindolizidine alkaloids have received an attention as potential therapeutic leads. To define the features of the molecule that are essential for cytotoxicity, we have synthesized and evaluated a series of phenanthroindolizidine alkaloid, antofine, analogues with different substituents on the phenanthrene ring. The systematic structure activity relationship studies elucidate the essential functional group requirement of phenanthrene ring, providing the basis for further development of phenanthroindolizidine alkaloids.

摘要

由于菲并吲哚里西啶生物碱具有深刻的细胞毒性和有趣的生化特性,它们作为潜在的治疗先导物受到了关注。为了确定对细胞毒性至关重要的分子特征,我们合成并评估了一系列菲并吲哚里西啶生物碱安托非碱的类似物,这些类似物在菲环上带有不同的取代基。系统的构效关系研究阐明了菲环必需的官能团要求,为菲并吲哚里西啶生物碱的进一步开发提供了基础。

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