Synthesis and biological evaluation of 2-acyl analogues of paclitaxel (Taxol)

被引：71

作者：

Kingston, DGI ^{[1
]}

Chaudhary, AG

Chordia, MD

Gharpure, M

Gunatilaka, AAL

Higgs, PI

Rimoldi, JM

Samala, L

Jagtap, PG

Giannakakou, P

Jiang, YQ

Lin, CM

Hamel, E

Long, BH

Fairchild, CR

Johnston, KA

机构：

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

[2] NCI, Div Clin Sci, Med Branch, NIH, Bethesda, MD 20892 USA

[3] NCI, Frederick Canc Res & Dev Ctr, Div Canc Treatment & Diag,Dev Therapeut Program, Lab Drug Discovery Res & Dev, Frederick, MD 21702 USA

[4] Bristol Myers Squibb Pharmaceut Res Inst, Princeton, NJ USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1998年 / 41卷 / 19期

关键词：

D O I：

10.1021/jm980229d

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The anticancer drug paclitaxel (Taxol) has been converted to a large number of 2-debenzoyl-2-aroyl derivatives by three different methods. The bioactivities of the resulting analogues were determined in both tubulin polymerization and cytotoxicity assays, and several analogues with enhanced activity as compared with paclitaxel were discovered. Correlation of cytotoxicity in three cell lines with tubulin polymerization activity showed reasonable agreement. Among the cell lines examined, the closest correlation with antitubulin activity was observed with a human ovarian carcinoma cell line.

引用

页码：3715 / 3726

页数：12

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