Synthesis and biological evaluation of 2′-methyl taxoids derived from baccatin III and 14β-OH-baccatin III 1,14-carbonate

被引：17

作者：

Battaglia, A

Bernacki, RJ

Bertucci, C

Bombardelli, E

Cimitan, S

Ferlini, C

Fontana, G

Guerrini, A

Riva, A

机构：

[1] ISOF, Ist CNR Sintesi Organ & Fotoreatt, I-40129 Bologna, Italy

[2] Roswell Pk Canc Inst, Dept Pharmacol & Therapeut, Buffalo, NY 14263 USA

[3] Univ Bologna, Dipartimento Sci Farmaceut, I-40126 Bologna, Italy

[4] Indena SPA, I-20139 Milan, Italy

[5] Univ Cattolica Sacro Cuore, Dipartimento Ostet & Ginecol, Lab Farmacol Antineoplast, Rome, Italy

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2003年 / 46卷 / 23期

关键词：

TAXOL(R) ANALOGS; DERIVATIVES; EFFICIENT; TAXANES;

D O I：

10.1021/jm034146v

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 2'-methyl taxoids were synthesized and essayed for growth inhibition experiments conducted in human ovarian cancer cell line A2780wt and its counterparts A2780cis, A2780tax, and A2780adr, resistant to cisplatin, paclitaxel, and doxorubicin, respectively, to test the effect of this substituent on the antitumor activity. Additional experiments were performed on MCF-7 human breast cancer cell line and MCF7-R resistant to doxorubicin. In several cases these taxoids were more active than paclitaxel showing subnanomolar IC50 values.

引用

页码：4822 / 4825

页数：4

共 26 条

[1] New efficient synthesis of (3R,4S)-3-methyl-3-hydroxy-4-phenyl-β-lactam [J].