Chordia M D, Kingston D G, Hamel E, Lin C M, Long B H, Fairchild C A, Johnston K A, Rose W C
Department of Chemistry, Virginia Polytechnic Institute and State University, Blacksburg 24061-0212, USA.
Bioorg Med Chem. 1997 May;5(5):941-7. doi: 10.1016/s0968-0896(97)00035-7.
A number of paclitaxel analogues with a 5-membered A-ring (A-nor-paclitaxels, or (15-->1)-abeo-paclitaxels) have been prepared in order to determine whether analogues of this class might have improved bioactivity as compared with paclitaxel. Most of the compounds synthesized were less active than paclitaxel, but one analogue was equivalent to paclitaxel in a tubulin-assembly assay, and another analogue was more cytotoxic than paclitaxel in two different cell lines of the NCI screen.
为了确定与紫杉醇相比，这类类似物是否可能具有更高的生物活性，人们已制备了多种具有五元A环的紫杉醇类似物（A-去甲紫杉醇，或(15→1)-阿贝奥紫杉醇）。合成的大多数化合物活性低于紫杉醇，但有一种类似物在微管蛋白组装试验中的活性与紫杉醇相当，还有一种类似物在NCI筛选的两种不同细胞系中比紫杉醇具有更强的细胞毒性。
