The Identification of Perillyl Alcohol Glycosides with Improved Antiproliferative Activity
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- 作者：Nitin S. Nandurkar ; Jianjun Zhang ; Qing Ye ; Larissa V. Ponomareva ; Qing-Bai She ; Jon S. Thorson
- 刊名：Journal of Medicinal Chemistry
- 出版年：2014
- 出版时间：September 11, 2014
- 年：2014
- 卷：57
- 期：17
- 页码：7478-7484
- 全文大小：399K
- ISSN：1520-4804
文摘
A facile route to perillyl alcohol (POH) differential glycosylation and the corresponding synthesis of a set of 34 POH glycosides is reported. Subsequent in vitro studies revealed a sugar dependent antiproliferative activity and the inhibition of S6 ribosomal protein phosphorylation as a putative mechanism of representative POH glycosides. The most active glycoside from this cumulative study (4鈥?azido-<span class="smallcaps">dspan>-glucoside, PG9) represents one of the most cytotoxic POH analogues reported to date.