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.
journal_name
Arch Pharm (Weinheim)journal_title
Archiv der Pharmazieauthors
El-Gamal MI,Choi HS,Cho HG,Hong JH,Yoo KH,Oh CHdoi
10.1002/ardp.201000375subject
Has Abstractpub_date
2011-11-01 00:00:00pages
745-54issue
11eissn
0365-6233issn
1521-4184journal_volume
344pub_type
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