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牛油果衍生毒素 (+)-(R)-persin 类似物的合成及其在人乳腺癌细胞中的体外评价。

Synthesis and in vitro evaluation of analogues of avocado-produced toxin (+)-(R)-persin in human breast cancer cells.

机构信息

Auckland Cancer Society Research Centre, Faculty of Medical and Health Sciences, The University of Auckland, Private Bag 92019, Auckland 1142, New Zealand.

出版信息

Bioorg Med Chem. 2011 Dec 1;19(23):7033-43. doi: 10.1016/j.bmc.2011.10.006. Epub 2011 Oct 13.

Abstract

A structure-activity study of several new synthetic analogues of the avocado-produced toxin persin has been conducted, with compounds being evaluated for their cytostatic and pro-apoptotic effects in human breast cancer cells. A 4-pyridinyl derivative demonstrated activity comparable to that of the natural product, suggesting future directions for exploration of structure-activity relationships.

摘要

对几种新合成的鳄梨产生的毒素persin 类似物进行了构效关系研究,评估了这些化合物在人乳腺癌细胞中的细胞抑制和促凋亡作用。一种 4-吡啶基衍生物表现出与天然产物相当的活性,这表明了进一步探索构效关系的方向。

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