Design, Synthesis, and Antiproliferative Activity of 3,4-Diarylpyrazole-1-carboxamide Derivatives Against Melanoma Cell Line

Title
Design, Synthesis, and Antiproliferative Activity of 3,4-Diarylpyrazole-1-carboxamide Derivatives Against Melanoma Cell Line
Authors
엘가말최홍석조해국홍준희유경호오창현
Keywords
A375P; Antiproliferative activity; 3,4-Diarylpyrazole; Melanoma; 1H-Pyrazole-1-carboxamide
Issue Date
2011-11
Publisher
Archiv der Pharmazie
Citation
VOL 344, NO 11, 745-754
Abstract
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.
URI
http://pubs.kist.re.kr/handle/201004/40682
ISSN
0365-6233
Appears in Collections:
KIST Publication > Article
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