El-Gamal, Mohammed I. Jung, Myung-Ho Lee, Woong San Sim, Taebo Yoo, Kyung Ho Oh, Chang-Hyun 2024-01-20T16:32:43Z 2024-01-20T16:32:43Z 2022-01-10 2011-08 0223-5234 https://pubs.kist.re.kr/handle/201004/130102 Synthesis of a new series of diarylureas and diarylamides having 1H-pyrrolo[3,2-c]pyridine scaffold is described. Their in vitro antiproliferative activity against A375P human melanoma cell line was tested and the effect of substituents on pyrrolo[3,2-c]pyridine nucleus was investigated. The newly synthesized compounds, except three N-tolyl derivatives (8f, 9f, and 9h), generally showed superior activity against A375P to Sorafenib. Among all of these derivatives, compounds 8b, 8g, and 9a-e showed the highest potency against A375P with IC50 in nanomolar range. In addition, compounds 8d, 8e, 8h, 9g, 9i, and 9j were more potent than Sorafenib but with IC50 in micromolar range. Compounds 8b, 8g, 9b-d, and 9i demonstrated higher selectivity towards A375P compared with NIH3T3 fibroblasts. The most potent diarylurea 8g and diarylamide 9d were further tested and showed high potency over nine melanoma cell lines at the NCI. (C) 2011 Elsevier Masson SAS. All rights reserved. English ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER THERAPY INTERLEUKIN-2 DIAGNOSIS Design, synthesis, and antiproliferative activity of new 1H-pyrrolo[3,2-c]pyridine derivatives against melanoma cell lines Article 10.1016/j.ejmech.2011.04.031 1 EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, v.46, no.8, pp.3218 - 3226 EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 46 8 3218 3226 scie scopus 000292670000005 2-s2.0-79958278972 Chemistry, Medicinal Pharmacology & Pharmacy Article THERAPY INTERLEUKIN-2 DIAGNOSIS Pyrrolo[3,2-c]pyridine A375P Antiproliferative activity Melanoma Diarylurea Diarylamide