（+）-佛波醇酯A的合成研究。一系列高细胞毒性C（45-46）类似物的鉴定。

(+)-Phorboxazole A synthetic studies. Identification of a series of highly cytotoxic C(45-46) analogues.

作者信息

Smith Amos B, Razler Thomas M, Pettit George R, Chapuis Jean-Charles

机构信息

Department of Chemistry, Monell Chemical Senses Center, University of Pennsylvania, Philadelphia, Pennsylvania 19104, USA.

出版信息

Org Lett. 2005 Sep 29;7(20):4403-6. doi: 10.1021/ol051585a.

DOI:10.1021/ol051585a

PMID:16178544

Abstract

[structure: see text] Effective, scalable total syntheses and biological evaluation of six phorboxazole A analogues (1-6) have been achieved. Importantly, the C(45-46)-saturated, C(45-46)-alkenyl, and the C(45-46)-E-chloroalkenyl congeners (4, 5, and 6, respectively) reveal low nanomolar tumor cell growth inhibitory activity (GI50's) similar to or, in some cell lines, greater than that of the phorboxazoles across a diverse panel of human cancer cell lines.

摘要

[结构：见原文] 已完成六种佛波醇酯A类似物（1-6）的高效、可扩展的全合成及生物学评估。重要的是，C(45-46)饱和、C(45-46)烯基和C(45-46)-E-氯代烯基同系物（分别为4、5和6）在多种人类癌细胞系中显示出低纳摩尔水平的肿瘤细胞生长抑制活性（GI50），与佛波醇酯类似，在某些细胞系中活性更强。