Twenty eight 6,7-dihydrobenzo[f]benzo[4,5]imidazo[1,2-d][1,4]oxazepine derivatives were synthesized and evaluated their biological activities as PI3K inhibitors. Biological evaluation against four human tumor cell lines revealed that most target compounds showed impressively better antiproliferative activities than that of LY294002. Among these compounds, compound 25 exhibited the most potent and selective activity for PI3Kα, with the IC₅₀ value of 0.016 μM, an approximately 30-fold increase in comparison with LY294002, it also has an increased potency of approximately 11-fold for PI3Kβ. It indicated the potential of developing 6,7-dihydrobenzo[f]benzo[4,5]imidazo[1,2-d][1,4]oxazepine derivatives as the new PI3Kα selective inhibitors for tumor treatment.

合成了二十八个6,7-二氢苯并[ f ]苯并[4,5]咪唑并[1,2- d ] [1,4]奥氮平衍生物，并评估了它们作为PI3K抑制剂的生物学活性。对四种人类肿瘤细胞系的生物学评价显示，大多数目标化合物表现出比LY294002更好的抗增殖活性。在这些化合物中，化合物25对PI3Kα表现出最强的选择性活性，IC ₅₀值为0.016μM，与LY294002相比，增加了约30倍，对PI3Kβ的效力也增加了约11倍。它表明了开发6,7-二氢苯并[ f]苯并[4,5]咪唑并[1,2- d ] [1,4]奥氮平衍生物作为新型PI3Kα选择性抑制剂，可用于治疗肿瘤。