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源自生物合成代谢产物的格尔德霉素衍生物的合成及其抗癌活性

Synthesis and anticancer activity of geldanamycin derivatives derived from biosynthetically generated metabolites.

作者信息

Lee Kyeong, Ryu Jung S, Jin Yinglan, Kim Woncheol, Kaur Navneet, Chung Sang J, Jeon Yong-Jin, Park Joon-Tae, Bang Ji S, Lee Hong S, Kim Tae Y, Lee Jung J, Hong Young-Soo

机构信息

Korea Research Institute of Bioscience & Biotechnology, 52 Eoeundong, Yuseonggu, Daejeon, 305-806, Korea.

出版信息

Org Biomol Chem. 2008 Jan 21;6(2):340-8. doi: 10.1039/b713407j. Epub 2007 Nov 30.

DOI:10.1039/b713407j
PMID:18175003
Abstract

A new series of geldanamycin derivatives were synthesized using a semi-synthetic approach involving genetically engineered biosynthetic intermediates. These analogues were then evaluated for anti-proliferation activity in human cancer cell lines, SK-Br3 and SK-Ov3. Most of the synthesized compounds exhibited potent in vitro anti-proliferation activity toward both cell lines. Such compounds potently inhibited the expression of the Hsp90 client protein ErbB2.

摘要

采用涉及基因工程生物合成中间体的半合成方法合成了一系列新的格尔德霉素衍生物。然后在人癌细胞系SK-Br3和SK-Ov3中评估这些类似物的抗增殖活性。大多数合成化合物对这两种细胞系均表现出强大的体外抗增殖活性。这些化合物强烈抑制热休克蛋白90（Hsp90）客户蛋白ErbB2的表达。

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