环杷明衍生物的合成与抗癌活性研究

Synthesis and anticancer activity studies of cyclopamine derivatives.

作者信息

Zhang Jianjun, Garrossian Massoud, Gardner Dale, Garrossian Arash, Chang Young-Tae, Kim Yun Kyung, Chang Cheng-Wei Tom

机构信息

Department of Chemistry and Biochemistry, Utah State University, 0300 Old Main Hill, Logan, UT 84322-0300, USA.

出版信息

Bioorg Med Chem Lett. 2008 Feb 15;18(4):1359-63. doi: 10.1016/j.bmcl.2008.01.017. Epub 2008 Jan 9.

DOI:10.1016/j.bmcl.2008.01.017

PMID:18221872

Abstract

A diversity-oriented synthesis has been developed for facile construction of a library of carbohydrate-cyclopamine conjugates. The synthetic protocol is suitable for generating cyclopamine derivatives with various structural motifs for exploring the desired activity. From this initial library, we have observed one derivative that exhibits improved activity against lung cancer cell as compared to cyclopamine.

摘要

已开发出一种以多样性为导向的合成方法，用于便捷构建碳水化合物 - 环杷明缀合物文库。该合成方案适用于生成具有各种结构基序的环杷明衍生物，以探索所需活性。从这个初始文库中，我们观察到一种衍生物，与环杷明相比，它对肺癌细胞表现出更高的活性。