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Synthesis of 1 H ‐Pyrazole‐1‐carboxamide Derivatives and Their Antiproliferative Activity against Melanoma Cell Line
Author(s) -
ElGamal Mohammed I.,
Sim Tae Bo,
Hong Jun Hee,
Cho JungHyuck,
Yoo Kyung Ho,
Oh ChangHyun
Publication year - 2011
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201000057
Subject(s) - carboxamide , pyrazole , melanoma , chemistry , cell culture , biological activity , stereochemistry , chemical synthesis , cell growth , structure–activity relationship , pharmacology , combinatorial chemistry , cancer research , in vitro , biochemistry , biology , genetics
Synthesis of a new series of 1 H ‐pyrazole‐1‐carboxamide derivatives is 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 newly synthesized compounds showed moderate activity against A375, compared with sorafenib. Among all of these derivatives, compound IIe which has N‐ methylpiperazinyl and phenolic moieties showed the most potent antiproliferative activity against A375 human melanoma cell line.