半合成
天然产物
全合成
微管
红豆杉
抗有丝分裂剂
化学
微管蛋白
生物
立体化学
生物化学
植物
细胞生物学
作者
K. C. Nicolaou,Zhen Yang,J. J. Liu,Hiroshi Ueno,P. G. Nantermet,R. Kiplin Guy,Christopher F. Claiborne,J. Renaud,Elias A. Couladouros,K. Paulvannan,Erik J. Sorensen
出处
期刊:Nature
[Springer Nature]
日期:1994-02-01
卷期号:367 (6464): 630-634
被引量:1038
摘要
Taxol, a substance originally isolated from the Pacific yew tree (Taxus brevifolia) more than two decades ago, has recently been approved for the clinical treatment of cancer patients. Hailed as having provided one of the most significant advances in cancer therapy, this molecule exerts its anticancer activity by inhibiting mitosis through enhancement of the polymerization of tubulin and consequent stabilization of microtubules. The scarcity of taxol and the ecological impact of harvesting it have prompted extension searches for alternative sources including semisynthesis, cellular culture production and chemical synthesis. The latter has been attempted for almost two decades, but these attempts have been thwarted by the magnitude of the synthetic challenge. Here we report the total synthesis of taxol by a convergent strategy, which opens a chemical pathway for the production of both the natural product itself and a variety of designed taxoids.
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