一些天然和合成愈创木内酯的细胞毒性活性。
Cytotoxic activity of some natural and synthetic guaianolides.
作者信息
Bruno Maurizio, Rosselli Sergio, Maggio Antonella, Raccuglia Rosa Angela, Bastow Kenneth F, Lee Kuo-Hsiung
机构信息
Dipartimento di Chimica Organica, Università di Palermo, Viale delle Scienze, 90128 Palermo, Italy.
出版信息
J Nat Prod. 2005 Jul;68(7):1042-6. doi: 10.1021/np0500575.
PMID:16038545
Abstract
Several natural guaianolides and synthetic derivatives of repin (1) were tested and found to be active against tumor cell replication. Repin (1) and both mono- and di-halohydrin analogues (2, 7-9, 11, 12) showed significant antitumor potency. A more effective compound (17) was obtained by esterificating repin with the paclitaxel side chain.
摘要
对几种天然愈创木内酯类化合物以及瑞平（1）的合成衍生物进行了测试，发现它们对肿瘤细胞复制具有活性。瑞平（1）以及单卤代醇和二卤代醇类似物（2、7 - 9、11、12）均显示出显著的抗肿瘤效力。通过将瑞平与紫杉醇侧链酯化得到了一种更有效的化合物（17）。
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