埃博霉素结构修饰及其抗肿瘤活性研究进展

Structure modification and anticancer activity of epothilones

埃博霉素是从黏细菌的纤维堆囊菌发酵液中分离得到的大环内酯类化合物,它与紫杉醇具有相同的抑制肿瘤细胞生长作用,其构效关系是目前研究的热点之一。本文着重综述埃博霉素C2～C8区域、烯烃结构、C12～C13位置、环氧部分、R和S结构,以及噻唑侧链的化学修饰研究进展,阐述了修饰后对埃博霉素活性的影响,从而为设计高活性的埃博霉素类似物提供线索。

Epothilone, a class of macrocyclic lactones isolated from fermentation broth of strains of myxobacterium Sorangium cellulosum, has the same inhibitory mechanism on tumor cell growth as paclitaxel. The structure activity relationship of epothilone is the focus of current research, so the emphasis of this paper is laid on the modification of the C2-C8 region, alkene, C12-C13 site, epoxy area, R and S configuration, and thiazole side chain of epothilone, analyzes the influence of modification on its activity, and thus pro- vides some rules for rational design of high active epothilones.