1308319-71-2

Upstream product

• 616-79-5 2-amino-5-nitro-benzoic acid 
• 32618-85-2 6-Nitro-1H-quinazoline-2,4-dione 
• 74173-77-6 2,4-dichloro-6-nitro-quinazoline 
• 1308320-02-6 methyl 4-(2-(3-(4-trifluoromethylphenyl)ureido)-6-nitroquinazolin-4-ylamino)benzoate 
• 1308319-76-7 methyl 4-(2-chloro-6-nitroquinazolin-4-ylamino)benzoate 
• 1308319-96-1 methyl 4-(2-amino-6-nitroquinazolin-4-ylamino)benzoate 

Relevant academic research and scientific papers

2,4-disubstituted [...] compound, and its preparation, and pharmaceutical composition and use thereof

The invention discloses new 2,4-disubstituted quinazoline compounds and a preparation method, a medicinal composition and application thereof. The invention particularly relates to 2,4-disubstituted quinazoline compounds shown as a general formula I, medicinal salts thereof, precursors or derivatives thereof with the same biological function, a preparation method thereof, a composition containing one or more of the compounds, and application of the compounds in inhibiting activity of Pin1 enzyme, inhibiting activity of tumor growth and the like.

Synthesis and biological evaluation of novel quinazoline-derived human Pin1 inhibitors

A series of novel 2,4-disubstituted quinazoline derivatives were prepared and their inhibitory activities on hPin1 were evaluated. Of all the synthesized compounds, eight compounds displayed inhibitory activities with IC50 value at the level of 10-6 mol/L. Preliminary structure-activity relationships were analyzed in details and the binding mode of the titled compounds was predicted using FlexX algorithm. The design and optimization of novel small molecule Pin1 inhibitors will be guided by the results of this report.