Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3‑Kinase (PI3K) Inhibitors
dataset
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 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.
