Design and Synthesis of 3-(3-Chloro-4-substituted phenyl)-4-(pyridin-4-yl)-1H-pyrazole-1-1-carboxamide Derivatives and Their Antiproliferative Activity Against Melanoma Cell Line

Title
Design and Synthesis of 3-(3-Chloro-4-substituted phenyl)-4-(pyridin-4-yl)-1H-pyrazole-1-1-carboxamide Derivatives and Their Antiproliferative Activity Against Melanoma Cell Line
Authors
엘가말오창현
Keywords
Antiproliferative activity; 1H-Pyrazole-1-carboxamide; A375; Melanoma; 3,4-Diarylpyrazole
Issue Date
2011-03
Publisher
Bulletin of the Korean Chemical Society
Citation
VOL 32, NO 3, 821-828
Abstract
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.
URI
http://pubs.kist.re.kr/handle/201004/41276
ISSN
0253-2964
Appears in Collections:
KIST Publication > Article
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