Design, Synthesis, and Antiproliferative Activity of 3,4-Diarylpyrazole-1-carboxamide Derivatives Against Melanoma Cell Line
- Design, Synthesis, and Antiproliferative Activity of 3,4-Diarylpyrazole-1-carboxamide Derivatives Against Melanoma Cell Line
- 엘가말; 최홍석; 조해국; 홍준희; 유경호; 오창현
- A375P; Antiproliferative activity; 3,4-Diarylpyrazole; Melanoma; 1H-Pyrazole-1-carboxamide
- Issue Date
- Archiv der Pharmazie
- VOL 344, NO 11, 745-754
- 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.
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