654682-88-9

Upstream product

• 364-83-0 2',4'-difluoroacetophenone 
• 459-57-4 4-fluorobenzaldehyde 

Downstream Products

• 1224407-99-1 2,3-dibromo-1-(2,4-difluorophenyl)-3-(p-fluorophenyl)propan-1-one 

Relevant academic research and scientific papers

Multi-target weapons: diaryl-pyrazoline thiazolidinediones simultaneously targeting VEGFR-2 and HDAC cancer hallmarks

In anticancer drug discovery, multi-targeting compounds have been beneficial due to their advantages over single-targeting compounds. For instance, VEGFR-2 has a crucial role in angiogenesis and cancer management, whereas HDACs are well-known regulators o

Double-edged Swords: Diaryl pyrazoline thiazolidinediones synchronously targeting cancer epigenetics and angiogenesis

In the present study, two novel series of compounds incorporating naphthyl and pyridyl linker were synthesized and biological assays revealed 5-((6-(2-(5-(2-chlorophenyl)-3-(4-fluorophenyl)-4,5-dihydro-1H-pyrazol-1-yl)-2-oxoethoxy) naphthalene-2-yl)methylene)thiazolidine-2,4-dione (14b) as the most potent dual inhibitors of vascular endothelial growth factors receptor-2 (VEGFR-2) and histone deacetylase 4 (HDAC4). Compounds 13b, 14b, 17f, and 21f were found to stabilize HDAC4; where, pyridyl linker swords were endowed with higher stabilization effects than naphthyl linker. Also, 13b and 14b showed best inhibitory activity on VEGFR-2 as compared to others. Compound 14b was most potent as evident by in-vitro and in-vivo biological assessments. It displayed anti-angiogenic potential by inhibiting endothelial cell proliferation, migration, tube formation and also suppressed new capillary formation in the growing chick chorioallantoic membranes (CAMs). It showed selectivity and potency towards HDAC4 as compared to other HDAC isoforms. Compound 14b (25 mg/kg, i.p.) also indicated exceptional antitumor efficacy on in-vivo animal xenograft model of human colorectal adenocarcinoma (HT-29). The mechanism of action of 14b was also confirmed by western blot.

Synthesis and anti-inflammatory activity of fluorinated propanedione derivatives

A new series of five 1-(2′,4′-difluorophenyl)-3-(substituted phenyl)-1,3 propanediols from 2′,4′-difluorinated chalcones have been synthesized. All the compounds (20 mg/kg po) possess anti-inflammatory activity, as reflected by their ability to provide protection (70.00 - 93.00%) against carrageenan induced edema in rat paw. Standard indomethacin provided 79.00% protection at the same dose. The safety of these substituted propanediones are reflected by toxicity studies.

CHEMICAL COMPOUNDS

Compounds of formula (I):wherein variable groups are as defined within; for use in the inhibition of 11betaHSD1 are described