Synthesis and biological evaluation of C-3′NH/C-10 and C-2/C-10 modified paclitaxel analogues

被引：20

作者：

Baloglu, E

Hoch, JM

Chatterjee, SK

Ravindra, R

Bane, S

Kingston, DGI

机构：

[1] Virginia Polytech Inst & State Univ, Dept Chem, Blacksburg, VA 24061 USA

[2] SUNY Binghamton, Dept Chem, Binghamton, NY 13902 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2003年 / 11卷 / 07期

关键词：

D O I：

10.1016/S0968-0896(02)00608-9

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Concurrent modifications on the C-3'NH/C-10, and C-2/C-10 positions on paclitaxel were carried out as a way of investigating possible synergistic effects. The biological activities of these analogues were evaluated in both a microtubule assembly assay and human ovarian cancer (A2780) and prostate cancer (PC3) cytotoxicity assay. In some cases the doubly modified analogues were more active than would have been predicted based on the activity of the singly modified analogues, indicating probable synergistic effects. (C) 2003 Elsevier Science Ltd. All rights reserved.

引用

页码：1557 / 1568

页数：12

共 36 条

[1] Butitaxel analogues: Synthesis and structure-activity relationships [J].