135106-52-4

Upstream product

• 436-72-6 5-fluoroquinazolin-4(3H)-one 
• 124-41-4 sodium methylate 
• 1591-38-4 2-amino-6-methoxybenzamide 
• 54166-96-0 methyl 2-amino-6-methoxybenzoate 
• 463-52-5 formamidine 
• 875245-80-0 2-formylamino-6-methoxy-benzoic acid amide 

Downstream Products

• 379228-40-7 4-[(2-chloro-5-methoxyphenyl)amino]quinazolin-5-ol 
• 733017-07-7 4-(4'-trifluoromethylphenyl)-5-trifluoromethylsulfonyloxyquinazoline 
• 733017-08-8 4-(3'-nitrophenyl)-5-trifluoromethylsulfonyloxyquinazoline 
• 733017-01-1 5-methoxy-4-(4'-trifluoromethylphenyl)quinazoline 
• 733017-04-4 5-hydroxy-4-(4'-trifluoromethylphenyl)quinazoline 
• 733017-05-5 5-hydroxy-4-(3'-nitrophenyl)quinazoline 
• 733017-02-2 5-methoxy-4-(3'-nitrophenyl)quinazoline 
• 179246-14-1 4-chloro-5-methoxyquinazoline 

Relevant academic research and scientific papers

4- (IH-INDAZOL-S-YL-AMINO)-QUINAZOLINE COMPOUNDS AS ERBB RECEPTOR TYROSINE KINASE INHIBITORS FOR THE TREATMENT OF CANCER

A quinazoline derivative of the Formula I: wherein the substituents are as defined in the text for use in the production of an anti proliferative effect which effect is produced alone or in part by inhibiting erbB2 receptor tyrosine kinase in a warm blood

QUINAZOLINE DERIVATIVES AS ANTICANCER AGENTS

A quinazoline derivative of the Formula I: wherein the substituents are as defined in the text for use in the production of an anti proliferative effect which effect is produced alone or in part by inhibiting erbB2 receptor tyrosine kinase in a warm blood

N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy] -5-(tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor

Src family kinases (SFKs) are nonreceptor tyrosine kinases that are reported to be critical for cancer progression. We report here a novel subseries of C-5-substituted anilinoquinazolines that display high affinity and specificity for the tyrosine kinase domain of the c-Src and Abl enzymes. These compounds exhibit high selectivity for SFKs over a panel of recombinant protein kinases, excellent pharmacokinetics, and in vivo activity following oral dosing. N-(5-Chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine (AZD0530) inhibits c-Src and Abl enzymes at low nanomolar concentrations and is highly selective over a range of kinases. AZD0530 displays excellent pharmacokinetic parameters in animal preclinically and in man (t1/2 = 40 h). AZD0530 is a potent inhibitor of tumor growth in a c-Src-transfected 3T3-fibroblast xenograft model in vivo and led to a significant increase in survival in a highly aggressive, orthotopic model of human pancreatic cancer when dosed orally once daily. AZD0530 is currently undergoing clinical evaluation in man.

Synthesis of 4,5-diarylquinazolines: A system with cofacial aromatic rings. Diazines. Part 39

Using metallation reactions and Pd-catalyzed coupling, we report here two synthetic routes leading to eight new 4,5-di(hetero)arylquinazolines. Non-linear activity has been highlighted for some of these compounds with stacked aromatic rings.