El-Gamal, Mohammed I. Park, Yi Seul Chi, Dae Yoon Yoo, Kyung Ho Oh, Chang-Hyun 2024-01-20T12:02:30Z 2024-01-20T12:02:30Z 2022-01-10 2013-07 0223-5234 https://pubs.kist.re.kr/handle/201004/127897 A new series of diarylureas and diarylamides possessing 1,3,4-triarylpyrazole scaffold was designed and synthesized. Their in vitro antiproliferative activities against NCI-60 cell line panel were tested. Most of the compounds showed strong and broad-spectrum antiproliferative activities. Compound 18 exerted sub-micromolar IC50 values over all the subpanels of nine different cancer types. Its IC50 value over MDA-MB-435 melanoma cell line was 27 nM. Compounds 10-13, 22, and 23 possessing urea spacer exerted lethal effect over the NCI-60 panel with mean %inhibitions more than 100% in single-dose testing. Compounds 13 and 23 with urea linker and 3',5'-bis(trifluoromethyl)phenyl terminal ring showed the highest mean %inhibition over the NCI-60 panel in single-dose testing, and showed high potencies and broad-spectrum anticancer activities in five-dose testing. (C) 2013 Elsevier Masson SAS. All rights reserved. English ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER MELANOMA-CELL LINE ANTIPROLIFERATIVE ACTIVITY 1,3,4-TRIARYLPYRAZOLE SCAFFOLD DERIVATIVES DIARYLAMIDES DIARYLUREAS DISCOVERY New triarylpyrazoles as broad-spectrum anticancer agents: Design, synthesis, and biological evaluation Article 10.1016/j.ejmech.2013.04.067 1 EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, v.65, pp.315 - 322 EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 65 315 322 scie scopus 000322850100031 2-s2.0-84878411252 Chemistry, Medicinal Pharmacology & Pharmacy Article MELANOMA-CELL LINE ANTIPROLIFERATIVE ACTIVITY 1,3,4-TRIARYLPYRAZOLE SCAFFOLD DERIVATIVES DIARYLAMIDES DIARYLUREAS DISCOVERY Anticancer Cytotoxicity Diarylurea Diarylamide 1,3,4-Triarylpyrazole