来自杂交红豆杉（Taxus x media cv. Hicksii）的紫杉醇类似物。

Paclitaxel analogues from Taxus x media cv. Hicksii.

作者信息

Gabetta B, Fuzzati N, Orsini P, Peterlongo F, Appendino G, Vander Velde D G

机构信息

Indena S.p.A, via Don Minzoni 6, 20090 Settala (MI), Dipartimento di Scienza e Tecnologia del Farmaco, via Giuria 9, 10125 Torino, Italy.

出版信息

J Nat Prod. 1999 Feb;62(2):219-23. doi: 10.1021/np9802264.

DOI:10.1021/np9802264

PMID:10075745

Abstract

The roots of T. x media Rehd. cv. Hicksii gave three novel analogues of paclitaxel modified at the N-acyl residue (N-debenzoyl-N-alpha-methylbutyryl paclitaxel and N-debenzoyl-N-cinnamoyl paclitaxel, 1b and 1c, respectively) or at the ester group at C-2 (2-debenzoyl-2-tigloyl paclitaxel, 1d). Compounds 1b and 1d showed reduced cytotoxicity and tubulin binding compared to paclitaxel, while 1c retained substantial activity in these assays.

摘要

杂交鹅掌楸（T. x media Rehd. cv. Hicksii）的根产生了三种新型紫杉醇类似物，它们在N-酰基残基处（分别为N-去苯甲酰基-N-α-甲基丁酰基紫杉醇和N-去苯甲酰基-N-肉桂酰基紫杉醇，即1b和1c）或在C-2位的酯基处（2-去苯甲酰基-2-惕各酰基紫杉醇，即1d）进行了修饰。与紫杉醇相比，化合物1b和1d表现出降低的细胞毒性和微管蛋白结合能力，而1c在这些测定中保留了相当的活性。