Antiproliferative Diarylpyrazole Derivatives as Dual Inhibitors of the ERK Pathway and COX-2

Title
Antiproliferative Diarylpyrazole Derivatives as Dual Inhibitors of the ERK Pathway and COX-2
Authors
모하메드엘가말최홍석유경호백대진오창현
Keywords
ERK pathway; cyclooxygenase-2; 3,4-diarylpyrazole-1-carboxamide; anticancer; pyrazole; vicinal diaryl heterocycle
Issue Date
2013-09
Publisher
Chemical biology & drug design
Citation
VOL 82, NO 3, 336-347
Abstract
A series of 3,4-diarylpyrazole-1-carboxamide derivatives was designed and synthesized. A selected group of the target compounds was tested for in vitro antiproliferative activities over a panel of 60 cancer cell lines at the National Cancer Institute (NCI, Bethesda, MD, USA) at a single-dose concentration of 10 lM, and the four most active compounds 9a, 9l, 9n, and 10o were further tested in a five-dose testing mode to determine their IC50 values over the 60 cell lines. In addition, a selected group of target compounds were tested for inhibitory effect over cyclooxygenase isozymes. Compounds 9a, 9l, 9n, and 10o were also tested for MEK and ERK kinase inhibitory activity using Western blot assay. Compound 10o was selective toward melanoma cell line subpanel, and its antiproliferative activity may be attributed to selective cyclooxygenase- 2 inhibition and ERK pathway inhibition.
URI
http://pubs.kist.re.kr/handle/201004/46295
ISSN
17470277
Appears in Collections:
KIST Publication > Article
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