El-Din, Mahmoud M. Gamal El-Gamal, Mohammed I. Abdel-Maksoud, Mohammed S. Yoo, Kyung Ho Oh, Chang-Hyun 2024-01-20T07:04:46Z 2024-01-20T07:04:46Z 2022-01-10 2015-04-15 0960-894X https://pubs.kist.re.kr/handle/201004/125543 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. English Pergamon Press Ltd. MELANOMA-CELL LINE BIOLOGICAL EVALUATION ANTICANCER AGENTS 1,3,4-TRIARYLPYRAZOLE SCAFFOLD BEARING OXADIAZOLE KINASE INHIBITION MOLECULAR DOCKING DESIGN NUCLEUS MOIETY Synthesis and broad-spectrum antiproliferative activity of diarylamides and diarylureas possessing 1,3,4-oxadiazole derivatives Article 10.1016/j.bmcl.2015.03.001 1 Bioorganic & Medicinal Chemistry Letters, v.25, no.8, pp.1692 - 1699 Bioorganic & Medicinal Chemistry Letters 25 8 1692 1699 scie scopus 000352143600007 2-s2.0-84939647480 Chemistry, Medicinal Chemistry, Organic Pharmacology & Pharmacy Chemistry Article MELANOMA-CELL LINE BIOLOGICAL EVALUATION ANTICANCER AGENTS 1,3,4-TRIARYLPYRAZOLE SCAFFOLD BEARING OXADIAZOLE KINASE INHIBITION MOLECULAR DOCKING DESIGN NUCLEUS MOIETY Antiproliferative activity Diarylamides Diarylureas 1,3,4-Oxadiazole