Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3‑Kinase (PI3K) Inhibitors
2016-07-18T00:00:00Z (GMT) by
Three series of substituted pyrimidines were designed and synthesized. All target compounds were screened for kinase inhibitory activities against PI3Kα, and most IC<sub>50</sub> values were found within the nanomolar range. Compounds <b>5d</b> and <b>5p</b> displayed comparable activities relative to the positive control <b>5a</b>. <b>5p</b> also showed a significant isozyme selectivity (PI3Kβ/α). Furthermore, the cytotoxicities of these pyrimidines against human cancer cell lines were evaluated and the in vivo anticancer effect of <b>5d</b> was also tested.