Jung, Myung-Ho El-Gamal, Mohammed I. Abdel-Maksoud, Mohammed S. Sim, Taebo Yoo, Kyung Ho Oh, Chang-Hyun 2024-01-20T14:31:14Z 2024-01-20T14:31:14Z 2022-01-10 2012-07-01 0960-894X https://pubs.kist.re.kr/handle/201004/129075 A new series of diarylureas and diarylamides possessing 1H- pyrrolo[3,2-c]pyridine scaffold was designed and synthesized. Their in vitro antiproliferative activities against A375P human melanoma cell line and NCI-9 human melanoma cell line panel were tested. All the target compounds, except three amino derivatives 8g, h and 9h, demonstrated superior potencies against A375P to Sorafenib. In addition, compounds 8a and 9b-f demonstrated higher potencies than Vemurafenib against A375P. Compounds 8c and 9b were 7.50 and 454.90 times, respectively, more selective towards A375P melanoma cells over NIH3T3 fibroblasts. Furthermore, compounds 8d, e and 9a-d, f demonstrated very high potencies against the nine tested melanoma cell lines at the NCI. The bisamide derivatives 9a-c, f showed 2-digit nanomolar IC50 values over different cell lines of the NCI-9 melanoma cell lines. (C) 2012 Elsevier Ltd. All rights reserved. English Pergamon Press Ltd. DIARYLAMIDES DIARYLUREAS SORAFENIB DIAGNOSIS THERAPY Design, synthesis, and antiproliferative activity of new 1H-pyrrolo[3,2-c]pyridine derivatives against melanoma cell lines. Part 2 Article 10.1016/j.bmcl.2012.05.004 1 Bioorganic & Medicinal Chemistry Letters, v.22, no.13, pp.4362 - 4367 Bioorganic & Medicinal Chemistry Letters 22 13 4362 4367 scie scopus 000305278100030 2-s2.0-84862170286 Chemistry, Medicinal Chemistry, Organic Pharmacology & Pharmacy Chemistry Article DIARYLAMIDES DIARYLUREAS SORAFENIB DIAGNOSIS THERAPY Pyrrolo[3,2-c]pyridine A375P Antiproliferative activity Melanoma Diarylurea Diarylamide