Synthesis of 1H-Pyrazole-1-carboxamide Derivatives and Their Antiproliferative Activity against Melanoma Cell Line

Authors
El-Gamal, Mohammed I.Sim, Tae BoHong, Jun HeeCho, Jung-HyuckYoo, Kyung HoOh, Chang-Hyun
Issue Date
2011-03
Publisher
WILEY-V C H VERLAG GMBH
Citation
ARCHIV DER PHARMAZIE, v.344, no.3, pp.197 - 204
Abstract
Synthesis of a new series of 1H-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.
Keywords
REFRACTORY SOLID TUMORS; FACTOR RECEPTOR INHIBITOR; RAF KINASE; METASTATIC MELANOMA; PHASE-I; SORAFENIB; BAY-43-9006; THERAPY; PHARMACOKINETICS; INTERLEUKIN-2; REFRACTORY SOLID TUMORS; FACTOR RECEPTOR INHIBITOR; RAF KINASE; METASTATIC MELANOMA; PHASE-I; SORAFENIB; BAY-43-9006; THERAPY; PHARMACOKINETICS; INTERLEUKIN-2; A375; Antiproliferative activity; 3,4-Diarylpyrazole; Melanoma; 1H-Pyrazole-1-carboxamide
ISSN
0365-6233
URI
https://pubs.kist.re.kr/handle/201004/130555
DOI
10.1002/ardp.201000057
Appears in Collections:
KIST Article > 2011
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