Quinazoline-based kinase inhibitors: new synthetic approach and biological evaluation.

In the last few years, particular attention was given to 4-anilinoquinazoline derivates for their highly specific and potent antitumoral activity as tyrosine kinase inhibitors. This significant interest for this class of compounds leads our research group to perform a new strategy for the synthesis of the quinazolinic scaffold, with the aim to going over some disadvantages of the already known synthetic routes, in particular the lack of commercially available starting products. Reaction has been further performed and improved using microwave-assisted technique, leading both to an increase in total yields and to a reduction of reaction time and of work-up. The prepared quinazoline scaffolds are suitable to be easily functionalized in 4-position with various amino substituents, to obtain potential ATP analogues. The functionalized quinazolines have been submitted to biological assay on several kinase to evaluate their inhibitor activity.