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氯 Pestolide A,一种来自榕树拟盘多毛孢的具有前所未有的螺环缩酮骨架的抗肿瘤代谢产物。

Chloropestolide A, an antitumor metabolite with an unprecedented spiroketal skeleton from Pestalotiopsis fici.

作者信息

Liu Ling, Li Yan, Liu Shuchun, Zheng Zhihui, Chen Xulin, Zhang Hua, Guo Liangdong, Che Yongsheng

机构信息

Key Laboratory of Systematic Mycology & Lichenology, Institute of Microbiology, Chinese Academy of Sciences, Beijing 100190, People's Republic of China.

出版信息

Org Lett. 2009 Jul 2;11(13):2836-9. doi: 10.1021/ol901039m.

DOI:10.1021/ol901039m
PMID:19496604
Abstract

Chloropestolide A (1), a highly functionalized spiroketal with an unprecedented skeleton derived from a chlorinated bicyclo-[2.2.2]-oct-2-en-5-one ring and a 2,6-dihydroxy-4-methylbenzoic acid unit, has been isolated from the scale-up fermentation extract of Pestalotiopsis fici. The structure of 1 was elucidated by NMR spectroscopy and X-ray crystallography. 1 could be derived from the same Diels-Alder precursors as 2 and showed significant inhibitory effects on growth of two human cancer cell lines, HeLa and HT29, with GI(50) values of 0.7 and 4.2 microM, respectively.

摘要

氯 Pestolide A(1)是一种高度官能化的螺环缩酮,具有前所未有的骨架,其衍生自氯化双环[2.2.2] -辛-2-烯-5-酮环和2,6-二羟基-4-甲基苯甲酸单元,它是从榕树拟盘多毛孢的放大发酵提取物中分离得到的。1的结构通过核磁共振光谱和X射线晶体学得以阐明。1可能与2来自相同的狄尔斯-阿尔德前体,并且对两种人类癌细胞系HeLa和HT29的生长显示出显著的抑制作用,其GI(50)值分别为0.7和4.2微摩尔。

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