El-Gamal, Mohammed I. Choi, Hong Seok Cho, Hae-Guk Hong, Jun Hee Yoo, Kyung Ho Oh, Chang-Hyun 2024-01-20T16:02:10Z 2024-01-20T16:02:10Z 2022-01-10 2011-11 0365-6233 https://pubs.kist.re.kr/handle/201004/129823 Synthesis of a new series of 3,4-diarylpyrazole-1-carboxamide derivatives is described. Their antiproliferative activity against A375P human melanoma cell line was tested and the effect of substituents on the diarylpyrazole scaffold was investigated. The biological results indicated that five synthesized compounds (Ig, Ii, IIc, IIg, and IIh) exhibited similar activity to Sorafenib. In addition, three compounds (IIa, IIb, and IIi) were more potent than Sorafenib. Among all of these derivatives, compound IIa which has dimethylamino and phenolic moieties showed the most potent antiproliferative activity against A375P human melanoma cell line. Virtual screening was carried out through docking of the most potent compound IIa 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, Synthesis, and Antiproliferative Activity of 3,4-Diarylpyrazole-1-carboxamide Derivatives Against Melanoma Cell Line Article 10.1002/ardp.201000375 1 ARCHIV DER PHARMAZIE, v.344, no.11, pp.745 - 754 ARCHIV DER PHARMAZIE 344 11 745 754 scie scopus 000297549200007 2-s2.0-80355126271 Chemistry, Medicinal Chemistry, Multidisciplinary Pharmacology & Pharmacy Pharmacology & Pharmacy Chemistry Article REFRACTORY SOLID TUMORS FACTOR RECEPTOR INHIBITOR RAF KINASE METASTATIC MELANOMA PHASE-I BAY-43-9006 SORAFENIB THERAPY PHARMACOKINETICS INTERLEUKIN-2 A375P Antiproliferative activity 3,4-Diarylpyrazole 1H-Pyrazole-1-carboxamide Melanoma