Synthesis and broad-spectrum antiproliferative activity of diarylamides and diarylureas possessing 1,3,4-oxadiazole derivatives

Title
Synthesis and broad-spectrum antiproliferative activity of diarylamides and diarylureas possessing 1,3,4-oxadiazole derivatives
Authors
마흐무드 가말엘딘모하메드엘가말모하메드 사미르유경호오창현
Keywords
Antiproliferative activity; Diarylamides; Diarylureas; 1,3,4-Oxadiazole
Issue Date
2015-04
Publisher
Bioorganic & medicinal chemistry letters
Citation
VOL 25, NO 8, 1692-1699
Abstract
A series of diarylamides and diarylureas possessing 1,3,4-oxadiazole scaffold was designed and synthesized. Their in vitro antiproliferative activities were tested against a panel of 58 cell lines of nine 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. The diarylurea compound 2g possessing 4-chloro-3-(trifluoromethyl) phenyl terminal moiety showed the highest mean % inhibition value of about 100% over the 58-cell line panel at 10 mu M concentration. Also compounds 2h, 2l, 2m exhibited mean % inhibition over 90% at 10 mu M concentration. The IC50 value of compound 2b over SNB-75 CNS cancer cell line was 0.65 mu M. Compound 2h also exerted submicromolar IC50 values of 0.67, 0.80, and 0.87 mu M against PC-3 prostate cancer cell line, HCT-116 colon cancer cell line, and ACHN renal cancer cell line, respectively. Compound 2h showed comparable efficacy to Sorafenib. (C) 2015 Elsevier Ltd. All rights reserved.
URI
http://pubs.kist.re.kr/handle/201004/50732
ISSN
0960894X
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KIST Publication > Article
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