1309606-07-2

Upstream product

• 1309605-97-7 4-[3-(3-chloro-4-methoxyphenyl)-1H-pyrazol-4-yl] pyridine 
• 1309605-98-8 3-(3-chloro-4-methoxyphenyl)-N-(2-(dimethylamino)ethyl)-4-(pyridin-4-yl)-1H-pyrazole-1-carboxamide 
• 51-44-5 3,4-dichlorbenzoic acid 
• 37908-96-6 3-chloro-4-methoxy benzoic acid 
• 37908-98-8 methyl 3-chloro-p-anisate 

Relevant academic research and scientific papers

Antiproliferative diarylpyrazole derivatives as dual inhibitors of the ERK pathway and COX-2

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 μm, 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.

Design and synthesis of 3-(3-chloro-4-substituted phenyl)-4-(pyridin-4-yl)- 1Hpyrazole- 1-carboxamide derivatives and their antiproliferative activity against melanoma cell line

Design and synthesis of new 3,4-diarylpyrazole-1-carboxamide derivatives are 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 synthesized compounds showed moderate activity against A375, compared with Sorafenib. On the other hand, compounds Ia, Ie, IIb, and IIh were more potent than Sorafenib. In addition, compound IIa was equipotent to Sorafenib. Among all of these derivatives, compound IIb which has diethylamino and phenolic moieties showed the most potent antiproliferative activity against A375 human melanoma cell line. Virtual screening was carried out through docking of the most potent compound IIb into the domain of V600E-b-Raf and the binding mode was studied. Copyright