Broad-spectrum antiproliferative activity of a series of 6-(4-fluorophenyl)-5-(2-substituted pyrimidin-4-yl)imidazo[2,1-b]thiazole derivatives

Title
Broad-spectrum antiproliferative activity of a series of 6-(4-fluorophenyl)-5-(2-substituted pyrimidin-4-yl)imidazo[2,1-b]thiazole derivatives
Authors
오창현모하메드 사미르마흐무드 가말엘딘모하메드엘가말곽성신김현일
Keywords
Antiproliferative; Biological activity; Imidazo[2,1-b]thiazole; Broad-spectrum
Issue Date
2016-05
Publisher
Medicinal chemistry research
Citation
VOL 25, NO 5-833
Abstract
This article described the synthesis and in vitro antiproliferative activities a series of 6-(4-fluorophenyl)-5-(2-substituted pyrimidin-4-yl)imidazo[2,1-b]thiazole derivatives. The nine target compounds were tested for in vitro antitumor effect against a panel of 55 cell lines of nine different cancer types at the NCI, and their activities were compared with that of Sorafenib as a reference standard drug. Compounds 1d and 1e possessing terminal arylamide moiety exerted superior potencies than Sorafenib against different cancer cell lines. Both compounds were more potent than Sorafenib against UO-31 renal cancer cell line and MCF7 breast cancer cell line. Compound 1d was also more potent than Sorafenib against COLO 205 colon cancer cell line, and compound 1e showed higher potency than Sorafenib against OVCAR-3 ovarian cancer cell line and DU-145 prostate cancel cell line also. For instance, the IC50 value of compound 1e against DU-145 prostate cancer cell line was 1.04 mu M, which is threefold more potent than Sorafenib.
URI
http://pubs.kist.re.kr/handle/201004/65052
ISSN
1054-2523
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KIST Publication > Article
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