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Abstract
In the research for the development of molecularly targeted cancer therapeutics (e.g. kinase inhibitors) which is considered as an appealing approach to decrease the side effects, toxicity and resistance of the conventional chemotherapeutic agents, it was planned to develop new dual PI3K alpha/ mTOR inhibitors. Till now there is no approved drug of this class in the market, therefore the drug discovery in this area is still unmet the medical need. Thus in this study, thirty three new 2,4-disubstituted quinazoline derivatives , seventeen new 2,4-disubstituted pyrido[3,2-d]pyrimidine derivatives and nineteen new 2,4-disubstituted pyrido[2,3-d]pyrimidine derivatives were synthesized through straightforward short synthetic routes. All of the prepared compounds were evaluated for in vitro PI3K alpha/ mTOR inhibitory activity and some of the promising compounds were screened for in vitro cytotoxicity. Furthermore, the tested compounds were investigated for their PI3K alpha and mTOR binding interactions through molecular docking studies