Aplysinopsin analogs: Synthesis and anti-proliferative activity of substituted (Z)-5-(N-benzylindol-3-ylmethylene)imidazolidine-2,4-diones.
Aplysinopsin analogs: Synthesis and anti-proliferative activity of substituted (Z)-5-(N-benzylindol-3-ylmethylene)imidazolidine-2,4-diones.
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海兔素类似物：取代的 (Z)-5-(N-苄基吲哚-3-基亚甲基)咪唑烷-2,4-二酮的合成和抗增殖活性。
DOI：
10.1016/j.bmc.2010.03.054
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发表时间：
2010
影响因子：
3.5
通讯作者：
Crooks,PeterA
中科院分区：
文献类型：
--
作者：
ThirupathiReddy,Y;NarsimhaReddy,P;Koduru,Srinivas;Damodaran,Chendil;Crooks,PeterA
在微波辐射和常规加热方法下合成了一系列结构上与Aplysinopsin结构相关的取代(Z)-5-(N-benzylindol-3-ylmethylene)imidazolidine-2，4-dione(3)类似物，它们在吲哚和N-苄基上都含有多种取代基，并对它们的抗增殖活性进行了评价。类似物3f和3j对MCF-7细胞的IC50值分别为4.4和5.2μM，而5-氟尿嘧啶的IC50为15.2μM。
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 IC50values of 4.4 and 5.2μM, respectively, compared to 5-fluorouracil (IC50=15.2μM) against MCF-7 cells.