Synthesis and broad-spectrum antiproliferative activity of diarylamides and diarylureas possessing 1,3,4-oxadiazole derivatives
- Synthesis and broad-spectrum antiproliferative activity of diarylamides and diarylureas possessing 1,3,4-oxadiazole derivatives
- 마흐무드 가말엘딘; 모하메드엘가말; 모하메드 사미르; 유경호; 오창현
- Antiproliferative activity; Diarylamides; Diarylureas; 1,3,4-Oxadiazole
- Issue Date
- Bioorganic & medicinal chemistry letters
- VOL 25, NO 8, 1692-1699
- 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.
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