Design, synthesis and biological evaluation of novel condensed pyrrolo[1,2-c]pyrimidines featuring morpholine moiety as PI3Kα inhibitors

Novel series of morpholino-pyrimidopyrrolopyrimidines 6a-d, 8a-d and 10a,b, and morpholino-pyridopyrrolopyrimidine-2-carbonitriles 12a-e were designed and synthesized as PI3K inhibitors. Compounds 8a-d and 12a-e proved to be potent and selective PI3Kα inhibitors.