设计并合成含 2-亚氨基噻唑烷-4-酮结构的化合物作为有效的抗增殖剂。
Design and synthesis of 2-iminothiazolidin-4-one moiety-containing compounds as potent antiproliferative agents.
机构信息
Key Laboratory of Original New Drugs Design and Discovery of Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang, China.
出版信息
Arch Pharm (Weinheim). 2012 May;345(5):360-7. doi: 10.1002/ardp.201100064. Epub 2012 Jan 2.
A new series of 2,5-diaryliminothiazolidin-4-ones were designed and synthesized as potent antiproliferative agents. The antiproliferative activities of the 25 target compounds were evaluated against three cancer cell lines (A549, H460 and HT29) by MTT assay. Pharmacological data indicated that most of the compounds possessed moderate activity, some showed remarkable activity against one or more cell lines. As the most promising compound, 8s (with IC(50) values of 1.1, 0.01 and 1.3 µM against the A549, H460 and HT29 cell lines) was 1.1- to 270-fold more potent than the reference drug sorafenib. Furthermore, preliminary structure-activity relationships (SARs) were summarized to provide guidance for further design and discovery of 2-iminothiazolidin-4-one-based antiproliferative agents.
我们设计并合成了一系列新的 2,5-二芳基亚氨基-4-恶唑啉酮类化合物，作为强效的抗增殖剂。通过 MTT 法评估了 25 个目标化合物对三种癌细胞系（A549、H460 和 HT29）的抗增殖活性。药理数据表明，大多数化合物具有中等活性，一些化合物对一种或多种细胞系表现出显著的活性。作为最有前途的化合物 8s（对 A549、H460 和 HT29 细胞系的 IC50 值分别为 1.1、0.01 和 1.3 μM），其活性比对照药物索拉非尼高 1.1-270 倍。此外，总结了初步的构效关系（SAR），为进一步设计和发现基于 2-亚氨基噻唑烷-4-酮的抗增殖剂提供了指导。
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