Antiproliferative Diarylpyrazole Derivatives as Dual Inhibitors of the ERK Pathway and COX-2
- Antiproliferative Diarylpyrazole Derivatives as Dual Inhibitors of the ERK Pathway and COX-2
- 모하메드엘가말; 최홍석; 유경호; 백대진; 오창현
- ERK pathway; cyclooxygenase-2; 3,4-diarylpyrazole-1-carboxamide; anticancer; pyrazole; vicinal diaryl heterocycle
- Issue Date
- Chemical biology & drug design
- VOL 82, NO 3, 336-347
- 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.
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