New diarylureas and diarylamides containing 1,3,4-triarylpyrazole scaffold: Synthesis, antiproliferative evaluation against melanoma cell lines, ERK kinase inhibition, and molecular docking studies

Synthesis of a new series of diarylureas and diarylamides possessing 1,3,4-triarylpyrazole scaffold is described. Their in vitro antiproliferative activities against 9 human melanoma cell lines were tested. Compounds 12, 13, 15, and 21– 23 showed the highest potency against A375P melanoma cell line....

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Veröffentlicht in:	European journal of medicinal chemistry 2011-12, Vol.46 (12), p.5754-5762
Hauptverfasser:	Choi, Won-Kyoung, El-Gamal, Mohammed I., Choi, Hong Seok, Baek, Daejin, Oh, Chang-Hyun
Format:	Artikel
Sprache:	eng
Schlagworte:	1,3,4-Triarylpyrazole Antineoplastic agents Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology B-RAF kinase Biological and medical sciences Cell Line, Tumor Cell Proliferation - drug effects Diarylamide Diarylurea Drug Screening Assays, Antitumor ERK kinase General aspects Humans MAP Kinase Signaling System - drug effects Medical sciences Melanoma Melanoma - drug therapy Models, Molecular Pharmacology. Drug treatments Protein Kinase Inhibitors - chemical synthesis Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacology Proto-Oncogene Proteins B-raf - antagonists & inhibitors Proto-Oncogene Proteins B-raf - metabolism Pyrazoles - chemical synthesis Pyrazoles - chemistry Pyrazoles - pharmacology Structure-Activity Relationship
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