El-Gamal, Mohammed I. Choi, Hong Seok Yoo, Kyung Ho Baek, Daejin Oh, Chang-Hyun 2024-01-20T11:33:11Z 2024-01-20T11:33:11Z 2022-01-10 2013-09 1747-0277 https://pubs.kist.re.kr/handle/201004/127691 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 10m, 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. English WILEY CYCLOOXYGENASE-2 EXPRESSION CANCER-CELLS ENDOMETRIAL CANCER LUNG-CANCER MELANOMA MACROPHAGES DESIGN Antiproliferative Diarylpyrazole Derivatives as Dual Inhibitors of the ERK Pathway and COX-2 Article 10.1111/cbdd.12186 1 CHEMICAL BIOLOGY & DRUG DESIGN, v.82, no.3, pp.336 - 347 CHEMICAL BIOLOGY & DRUG DESIGN 82 3 336 347 scie scopus 000323376300011 2-s2.0-84882893600 Biochemistry & Molecular Biology Chemistry, Medicinal Biochemistry & Molecular Biology Pharmacology & Pharmacy Article CYCLOOXYGENASE-2 EXPRESSION CANCER-CELLS ENDOMETRIAL CANCER LUNG-CANCER MELANOMA MACROPHAGES DESIGN 3,4-diarylpyrazole-1-carboxamide anticancer cyclooxygenase-2 ERK pathway pyrazole vicinal diaryl heterocycle