阿朴西多辛类似物的合成及取代（Z）-5-（N-苯并吲哚-3-亚甲基）咪唑烷-2,4-二酮的抗增殖活性。

Aplysinopsin analogs: Synthesis and anti-proliferative activity of substituted (Z)-5-(N-benzylindol-3-ylmethylene)imidazolidine-2,4-diones.

机构信息

Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, KY 40536, USA.

出版信息

Bioorg Med Chem. 2010 May 15;18(10):3570-4. doi: 10.1016/j.bmc.2010.03.054. Epub 2010 Mar 27.

DOI:10.1016/j.bmc.2010.03.054

PMID:20403701

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3726003/

Abstract

A series of substituted (Z)-5-(N-benzylindol-3-ylmethylene)imidazolidine-2,4-dione (3) analogs structurally related to aplysinopsin, and that incorporate a variety of substituents in both the indole and N-benzyl moieties have been synthesized under microwave irradiation and conventional heating methods These analogs were evaluated for their anti-proliferative activity against MCF-7 and MDA-231 breast cancer cell lines, and A549 and H460 lung cancer cell lines. Two analogs, 3f and 3j had IC(50) values of 4.4 and 5.2microM, respectively, compared to 5-fluorouracil (IC(50)=15.2microM) against MCF-7 cells.

摘要

一系列取代的（Z）-5-（N-苯并吲哚-3-亚甲基）咪唑烷-2,4-二酮（3）类似物与阿普里辛类似，并且在吲哚和 N-苄基部分都包含各种取代基，已经通过微波辐射和常规加热方法合成。这些类似物针对 MCF-7 和 MDA-231 乳腺癌细胞系以及 A549 和 H460 肺癌细胞系的抗增殖活性进行了评估。与 5-氟尿嘧啶（IC50=15.2μM）相比，两种类似物 3f 和 3j 对 MCF-7 细胞的 IC50 值分别为 4.4 和 5.2μM。