Koh, Eun Jeong El-Gamal, Mohammed I. Oh, Chang-Hyun Lee, So Ha Sim, Taebo Kim, Garam Choi, Hong Seok Hong, Jun Hee Lee, Sang-gi Yoo, Kyung Ho 2024-01-20T11:02:24Z 2024-01-20T11:02:24Z 2021-09-05 2013-12 0223-5234 https://pubs.kist.re.kr/handle/201004/127400 Synthesis of a new series of diarylureas and diarylamides possessing 4-aryl-8-amino(acetamido)quinoline scaffold is described. Their in vitro antiproliferative activities against ten melanoma cell lines were tested. Compounds 11, 21, 3c, and 4c showed the highest potency against A375P cell line with IC50 values in sub-micromolar scale. Compound 4c was equipotent to Vemurafenib against A375P. In addition, compounds 11, 2a, and 21 showed high potency over the NCI-9 tested melanoma cell line panel. The IC50 values of compounds 11 and 21 were in 2-digit nanomolar scale over four and five cell lines, respectively. Compound 21 showed high, dose-dependent inhibition of ERK kinase. ADME profiling showed that compounds 11, 21, 3c, 4c, and 5b are estimated to be orally bioavailable. (C) 2013 Elsevier Masson SAS. All rights reserved. English ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER DERIVATIVES DESIGN DISCOVERY DIAGNOSIS THERAPY BRAF New diarylamides and diarylureas possessing 8-amino(acetamido) quinoline scaffold: Synthesis, antiproliferative activities against melanoma cell lines, kinase inhibition, and in silico studies Article 10.1016/j.ejmech.2013.06.060 1 EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, v.70, pp.10 - 21 EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 70 10 21 scie scopus 000330554400002 2-s2.0-84885358486 Chemistry, Medicinal Pharmacology & Pharmacy Article DERIVATIVES DESIGN DISCOVERY DIAGNOSIS THERAPY BRAF Antiproliferative activity Diarylamide Diarylurea ERK kinase Melanoma Quinoline