期刊
MEDICINAL CHEMISTRY RESEARCH
卷 25, 期 5, 页码 824-833出版社
SPRINGER BIRKHAUSER
DOI: 10.1007/s00044-016-1529-7
关键词
Antiproliferative; Biological activity; Broad-spectrum; Imidazo[2,1-b]thiazole
资金
- Korea Institute of Science and Technology (KIST), KIST Project [2E24680]
- Ministry of Science, ICT & Future Planning, Republic of Korea [2E26230] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
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.
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