Broad-Spectrum Antiproliferative Activity of Diarylureas and Diarylamides Possessing Pyrrolo[3,2-c]Pyridine Scaffold
Broad-Spectrum Antiproliferative Activity of Diarylureas and Diarylamides Possessing Pyrrolo[3,2-c]Pyridine Scaffold作者机构：Center for Biomaterials Korea Institute of Science and Technology Seou1130650 Republic of Korea Department of Biomolecular Science University of Science and Technology Daejeon 305333 Republic of Korea Department of Medicinal Chemistry Faculty of Pharmacy Mansoura 35516 Egypt Chemical Kinomics Research Center Korea Institute of Science and Technology Seoul 130650 Republic of Korea
出 版 物：《Journal of Pharmacy and Pharmacology》 (药剂与药理学（英文版）)
年 卷 期：2014年第2卷第3期
页 面：157-169页
学科分类：1007[医学-药学(可授医学、理学学位)] 10[医学]
主 题：Anticancer antiproliferative diarylamide diarylurea pyrrolo[3 2-c]pyridine.
摘 要：A series of diarylureas and diarylamides possessing pyrrolo[3,2-c]pyridine scaffold was designed and synthesized. Their in vitro antiproliferative activities were tested against a panel of 49 cell lines of eight different cancer types at the NCI and compared with Sorafenib as a reference compound. Most of the compounds showed strong and broad-spectrum antiproliferative activities with superior potencies to Sorafenib. Compounds 8a, 9d and 9f showed lethal effect with mean %inhibition more than 100% over the 49 tested cell lines. In addition, the mean %inhibition results of compounds 8d, 8e, 9e, 9g and 9h were more than 80%. And most of the IC50 values of the target compounds were in submicromolar scale. Compounds 8a, 9b and 9e demonstrated high selectivity towards cancer cell lines compared with NIH3T3 fibroblasts.
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