Synthesis and biological evaluation of N-(2, 3-dimethyl-2H-indazol-6-yl) -2-methylpyrimidinediamine derivatives

OBJECTIVE: To synthesize N-(2, 3-dimethyl-2H-indazol-6-yl) -2-methylpyrimidinediamine derivatives and determine their antitumor activities in vitro. METHODS: Basing on the marketed multi-target antitumor agent, pazopanib, the objective substances were designed and synthesized according to the principle of fragment-based drug discovery. The antitumor activities in vitro of the synthesized compounds were evaluated by MTT method. RESULTS: Fourteen derivatives were synthesized. Their structures were identified by ¹H-NMR, MS and elemental analysis. CONCLUSION: It is shown that most of the synthesized compounds have antitumor activities, among which compound B1 and B2 show better antitumor activity than the positive control.