845-05-6

Upstream product

• 401-78-5 3-bromo-1-trifluoromethylbenzene 
• 536-45-8 sodium anisate 
• 2251-65-2 3-(Trifluoromethyl)benzoyl chloride 
• 454-92-2 3-(trifluoromethyl)benzoic acid 
• 100-66-3 methoxybenzene 

Downstream Products

• 62519-54-4 3-(4-methoxy-phenyl)-3-(3-trifluoro-methyl-phenyl)-propionic acid ethyl ester 
• 6615-93-6 2-Brom-1-methoxyphenyl-2-phenyl-1-(3-trifluormethyl-phenyl)-aethylen 
• 66938-64-5 (4-Amino-3-nitro-phenyl)-(3-trifluoromethyl-phenyl)-methanone 
• 6615-92-5 1-Methoxyphenyl-2-phenyl-1-(3-trifluormethyl-phenyl)-aethylen 
• 2560-61-4 4',4''-Dimethoxy-3,3'-bis-trifluormethyl-benzpinakon 
• 65214-64-4 4'-Methoxy-3-trifluormethyl-benzhydrol 
• 66938-44-1 (4-Methoxy-3-nitro-phenyl)-(3-trifluoromethyl-phenyl)-methanone 
• 732-55-8 (4-hydroxyphenyl)(3-(trifluoromethyl)phenyl)methanone 

Relevant academic research and scientific papers

Synthesis and structure-activity relationship for new series of 4-phenoxyquinoline derivatives as specific inhibitors of platelet-derived growth factor receptor tyrosine kinase

We discovered a new series of 4-phenoxyquinoline derivatives as potent and selective inhibitors of the platelet-derived growth factor receptor (PDGFr) tyrosine kinase. We researched the highly potent and selective inhibitors on the basis of both PDGFr and epidermal growth factor receptor (EGFr) inhibitory activity. First, we found a compound, Ki6783 (1), which inhibited PDGFr autophosphorylation at 0.13 μM, but it did not inhibit EGFr autophosphorylation at 100 μM. After extensive explorations, we found the two desired compounds, Ki6896 (2) and Ki6945 (3), which are substituted by benzoyl and benzamide at the 4-position of the phenoxy group on 4-phenoxyquinoline, respectively. These inhibitory activities were 0.31 and 0.050 μM, respectively, but neither of them inhibited EGFr autophosphorylation at 100 μM. We further investigated the profile of both compounds toward various tyrosine and serine/threonine kinases. The three compounds specifically inhibited PDGFr rather than the other kinases.

Quinoline and quinazoline derivatives inhibiting platelet-derived growth factor receptor autophosphorylation and pharmaceutical compositions containing the same

The present invention relates to novel quinoline derivatives and quinazoline derivatives represented by the following formula (I): STR1 [wherein R 1 and R 2 are each independently H or C 1 -C 4 -alkyl, or R 1 and R 2 together form C 1 -C 3 -alkylene, X is O, S or CH 2, W is CH or N, and Q is a substituted aryl group or substituted heteroaryl group] and their pharmaceutically acceptable salts, having platelet-derived growth factor receptor autophosphorylation inhibitory activity, to pharmaceutical compositions containing these compounds, and to methods for the treatment of diseases associated with abnormal cell growth such as tumors.

Polycyclic compounds

Compounds of the formula (II): STR1 and pharmaceutically acceptable salts thereof, wherein R1 is phenyl or naphthyl or substituted phenyl or naphthyl group; R2 is: STR2 wherein R5 is hydrogen or C1-6 alkyl, R6 is hydrogen or C1-6 alkyl, phenyl, tolyl or benzyl and R7 is hydrogen; R3 and R4 are each hydrogen atom or C1-4 alkyl, and X is CO, CHOH, CHCI or C=C R8 R9 wherein R8 and R9 are each hydrogen or C1-4 alkyl; or CR10 OH or CHR10, wherein R10 is C1-4 alkyl, have been found to be mood-modifying agents and anorexic agents.