Synthesis and biological activity of 3′-alkyl- and 3′-alkenyl-3′-dephenyldocetaxels

Iwao Ojima*, Olivier Duclos, Scott D. Kuduk, Chung-Ming Sun, John C. Slater, François Lavelle, Jean M. Veith, Ralph J. Bernacki

*此作品的通信作者

研究成果: Article同行評審

51 引文 斯高帕斯(Scopus)

摘要

3-Alkyl- and 3′-alkenyl-3′-dephenyldocetaxels are synthesized from 10-deacetylbaccatin III based on the β-lactam synthon method in good yields. The cytotoxicity of the new taxoids are evaluated against different human tumor cell lines and their ability to inhibit the microtubules disassembly examined. The 3′-isobutenyl, 3′-crotyl, and 3′-isobutyl analogs possess very strong cytotoxicity as well as antitumor activity in vivo. 3′-Isobutenyl- as well as 3′-crotyl-3′-dephenyl-10-acetyldocetaxel shows ca. 20 times stronger activity against an adriamycin-resistant human breast cancer cell line (MCF7-R) than those o docetaxel and paclitaxel.

原文English
頁(從 - 到)2631-2634
頁數4
期刊Bioorganic and Medicinal Chemistry Letters
4
發行號21
DOIs
出版狀態Published - 10 十一月 1994

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