Versatile synthesis of new cytotoxic agents structurally related to hemiasterlins
作者:Daniele Simoni、Ray M. Lee、David E. Durrant、Nai-Wen Chi、Riccardo Baruchello、Riccardo Rondanin、Cinzia Rullo、Paolo Marchetti
DOI:10.1016/j.bmcl.2010.03.098
日期:2010.6
Ag2O-promoted nucleophilic substitution on a common precursor, a chiral non-racemic 2-bromoacyl derivative. Simple variation of nucleophile substituents allows a rapid and stereocontrolled development of new series of derivatives. Some reported compounds showed potent biological activity as growth inhibitors of cancer cell lines and tubulin polymerization inhibitors.
已经合成了抗有丝分裂三肽半甾醇的代表性结构类似物系列。该合成策略的关键步骤包括在共同的前体(手性非外消旋2-溴酰基衍生物)上进行Ag 2 O促进的亲核取代。亲核试剂取代基的简单变化允许快速和立体控制的新系列衍生物的开发。一些报道的化合物作为癌细胞系的生长抑制剂和微管蛋白聚合抑制剂表现出强大的生物学活性。