jm6b00235_si_001.pdf (1.92 MB)
Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3‑Kinase (PI3K) Inhibitors
journal contribution
posted on 2016-07-18, 00:00 authored by Ji-Quan Zhang, Yong-Jie Luo, Yan-Shi Xiong, Yang Yu, Zheng-Chao Tu, Zi-Jie Long, Xiao-Ju Lai, Hui-Xuan Chen, Yu Luo, Jiang Weng, Gui LuThree series of substituted
pyrimidines were designed and synthesized. All target compounds were
screened for kinase inhibitory activities against PI3Kα, and
most IC50 values were found within the nanomolar range.
Compounds 5d and 5p displayed comparable
activities relative to the positive control 5a. 5p 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 5d was also tested.