N- 烷基-3- 羟基-3-(2-亚氨基-3-甲基-5-氧代咪唑烷-4-基)吲哚啉-2-酮类似物的合成及体外评价作为潜在的抗癌剂。
Synthesis and in vitro evaluation of N-alkyl-3-hydroxy-3-(2-imino-3-methyl-5-oxoimidazolidin-4-yl)indolin-2-one analogs as potential anticancer agents.
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 Lett. 2010 Aug 1;20(15):4468-71. doi: 10.1016/j.bmcl.2010.06.042. Epub 2010 Jun 10.
Abstract
A series of novel 3-hydroxy-3-(2-imino-3-methyl-5-oxoimidazolidin-4-yl)indolin-2-one analogs (3) have been synthesized under microwave irradiation and conventional heating methods. These analogs were evaluated for in vitro cytotoxicity against a panel of 57 human tumor cell lines. Compound 3o had GI(50) values of 190 nM and 750 nM against A549/ATTC non-small cell lung cancer and LOX IMVI melanoma cell lines, respectively, and both 3n and 3o exhibited GI(50) values ranging from 2 to 5 microM against CCRF-CEM, HL-60(TB), K-562, MOLT-4, and RPMI-8226 leukemia cell lines. These results indicate that N-4-methoxybenzyl-3-hydroxy-(2-imino-3-methyl-5-oxo-4-yl)indolin-2-one analogs may be useful leads for anticancer drug development.
摘要
已经通过微波辐射和常规加热方法合成了一系列新型 3-羟基-3-(2-亚氨基-3-甲基-5-氧代咪唑烷-4-基)吲哚啉-2-酮类似物(3)。对这些类似物进行了体外细胞毒性评估，针对 57 个人类肿瘤细胞系进行了评估。化合物 3o 对 A549/ATTC 非小细胞肺癌和 LOX IMVI 黑色素瘤细胞系的 GI(50)值分别为 190 nM 和 750 nM，而 3n 和 3o 对 CCRF-CEM、HL-60(TB)、K-562、MOLT-4 和 RPMI-8226 白血病细胞系的 GI(50)值均在 2 到 5 microM 之间。这些结果表明，N-4-甲氧基苄基-3-羟基-(2-亚氨基-3-甲基-5-氧代-4-基)吲哚啉-2-酮类似物可能是抗癌药物开发的有用先导物。
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