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目的寻找具有新型骨架结构的磷脂酰肌醇3激酶(PI3K)抑制剂。方法基于活性化合物,利用“杂交”设计原理,设计和合成了系列4-吗啉喹唑啉类衍生物。结果目标化合物经1HNMR、质谱确证结构,并评价了其对Rh30细胞的增殖抑制活性。结论大部分化合物具有较好的抑制活性,化合物8b的活性最强,其IC50达0.8μmol.L-1。4-吗啉喹唑啉是一类新型的PI3K抑制剂骨架,值得进一步进行结构修饰研究。
Aim To find a phosphatidylinositol 3 - kinase (PI3K) inhibitor with novel scaffold structure. Methods Based on the active compounds, a series of 4-morpholinoquinazoline derivatives were designed and synthesized based on the “” hybridization design principle. Results The target compounds were confirmed by 1HNMR and mass spectrometry. Their inhibitory activities on Rh30 cells were evaluated. Conclusion Most of the compounds have good inhibitory activity, and compound 8b has the strongest activity with an IC50 of 0.8μmol.L-1.4-morpholquinazoline is a new type of PI3K inhibitor scaffold, which deserves further structural modification the study.