Reported herein are efforts to profile 4-aryl-N-phenylpyrimidin-2-amines in terms of their anti-cancer activity towards non small-cell lung carcinoma (NSCLC) cells. We have synthesized new 4-aryl-N-phenylpyrimidin-2-amines and assessed them in terms of their cytotoxicity (A549, NCI-H187, MCF7, Vero & KB) and physicochemical properties (logD_7.4 and solubility). 13f and 13c demonstrated potent anti-cancer activity in A549 cells (0.2 µM), compared to 0.4 μM for the NSCLC drug Doxorubicin. 13f also displayed low experimental logD_7.4 (2.9) and the best solubility (∼40 μM). Compounds 13b and 13d showed the best balance of A549 anti-cancer activity and selectivity. 13g showed good activity and selectivity comparable with the anti-cancer drug Doxorubicin.

本文报道了关于4-芳基-N-苯基嘧啶-2-胺对非小细胞肺癌（NSCLC）细胞的抗癌活性的研究。我们合成了新的4-芳基-N-苯基嘧啶-2-胺，并根据其细胞毒性（A549，NCI-H187，MCF7，Vero和KB）和理化性质（logD _7.4和溶解度）对其进行了评估。与NSCLC药物阿霉素的0.4μM相比，图13f和13c在A549细胞（0.2μM）中显示出了强大的抗癌活性。13f还显示出较低的实验logD _7.4（2.9）和最佳溶解度（〜40μM）。化合物13b和13d显示出A549抗癌活性和选择性的最佳平衡。13g显示出与抗癌药阿霉素相当的活性和选择性。