El-Gamal, Mohammed I. Oh, Chang-Hyun 2024-01-20T17:30:54Z 2024-01-20T17:30:54Z 2022-01-10 2011-03-20 0253-2964 https://pubs.kist.re.kr/handle/201004/130517 Design and synthesis of new 3,4-diarylpyrazole-1-carboxamide derivatives are described. Their antiproliferative activity against A375 human melanoma cell line was tested and the effect of substituents on the diarylpyrazole scaffold was investigated. The pharmacological results indicated that most of the synthesized compounds showed moderate activity against A375, compared with Sorafenib. On the other hand, compounds Ia, Ie, IIb, and IIh were more potent than Sorafenib. In addition, compound IIa was equipotent to Sorafenib. Among all of these derivatives, compound IIb which has diethylamino and phenolic moieties showed the most potent antiproliferative activity against A375 human melanoma cell line. Virtual screening was carried out through docking of the most potent compound IIb into the domain of V600E-b-Raf and the binding mode was studied. English WILEY-V C H VERLAG GMBH REFRACTORY SOLID TUMORS FACTOR RECEPTOR INHIBITOR RAF KINASE METASTATIC MELANOMA PHASE-I BAY-43-9006 SORAFENIB THERAPY PHARMACOKINETICS INTERLEUKIN-2 Design and Synthesis of 3-(3-Chloro-4-substituted phenyl)-4-(pyridin-4-yl)-1H-pyrazole-1-carboxamide Derivatives and Their Antiproliferative Activity Against Melanoma Cell Line Article 10.5012/bkcs.2011.32.3.821 1 BULLETIN OF THE KOREAN CHEMICAL SOCIETY, v.32, no.3, pp.821 - 828 BULLETIN OF THE KOREAN CHEMICAL SOCIETY 32 3 821 828 scie scopus kci 000288832700012 2-s2.0-79953242277 Chemistry, Multidisciplinary Chemistry Article REFRACTORY SOLID TUMORS FACTOR RECEPTOR INHIBITOR RAF KINASE METASTATIC MELANOMA PHASE-I BAY-43-9006 SORAFENIB THERAPY PHARMACOKINETICS INTERLEUKIN-2 Antiproliferative activity 1H-Pyrazole-1-carboxamide 3,4-Diarylpyrazole A375 Melanoma