950525-41-4

Upstream product

• 108-89-4 picoline 
• 96826-41-4 methyl 3-chloro-5-methoxybenzoate 

Downstream Products

• 950525-42-5 4-[3-(3-chloro-5-methoxyphenyl)-1H-pyrazol-4-yl]pyridine 

Relevant academic research and scientific papers

Discovery of highly potent V600E-B-RAF kinase inhibitors: Molecular modeling study

A series of 20 triarylpyrazole derivatives containing amide or urea linker have been synthesized. Their in vitro antiproliferative activity against NCI-60 cancer cell lines panel has been reported. Upon investigating the mechanism of action at molecular l

Synthesis, in vitro antiproliferative activity, and kinase inhibitory effects of pyrazole-containing diarylureas and diarylamides

Twenty pyrazole-containing diarylureas and diarylamides were designed and synthesized. They were tested for in vitro antiproliferative activity over a 58-cancer cell line panel at the NCI, USA. The diarylurea derivatives 1b-e and 1g exerted the strongest

Synthesis and inhibitory effects of triarylpyrazoles on LPS-induced NO and PGE2 productions in RAW 264.7 macrophages

Abstract: The inhibition of nitric oxide and prostaglandin E2 productions is a very interesting research topic in the field of anti-inflammatory drug development. In the current study, a new series of 1,3,4-triarylpyrazole derivatives was synth

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.

Synthesis of 1H-Pyrazole-1-carboxamide derivatives and their antiproliferative activity against melanoma cell line

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.

PYRAZOLE COMPOUNDS

The present invention is directed to compounds of Formula (I), and to salts and solvates thereof, their synthesis, and their use as Raf inhibitors.