Broad-Spectrum Antiproliferative Activity of Diarylureas and Diarylamides Possessing Pyrrolo[3,2-c]Pyridine Scaffold

Title
Broad-Spectrum Antiproliferative Activity of Diarylureas and Diarylamides Possessing Pyrrolo[3,2-c]Pyridine Scaffold
Authors
아쉬라푸딩모하메드엘가말모하메드 사미르마흐무드 가말엘딘유경호오창현
Keywords
Anticancer; antiproliferative; diarylamide; diarylurea; pyrrolo[3,2-c]pyridine
Issue Date
2014-03
Publisher
Journal of Pharmacy and Pharmacology
Citation
VOL 2, 157-169
Abstract
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.
URI
http://pubs.kist.re.kr/handle/201004/48269
ISSN
23282150
Appears in Collections:
KIST Publication > Article
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