Novel 2,4-Diarylaminopyrimidine Derivatives Containing Pyridine Moiety:Design,Synthesis,Crystal Structure and Biological Evaluation

摘要

A series of 2,4-diarylaminopyrimidine derivatives containing pyridine structure were designed and synthesized.The crystal structures of compounds 5d and 5e were obtained from X-ray diffraction.The crystal structure of 5d (C_(25)H_(20)Cl FN_(6)O_(2)) belongs to the monoclinic system,space group P2_(1)/c with a=11.0500(10),b=18.3045(17),c=13.5646(9)?andβ=122.806(5)°.5e (C_(25)H_(19)Cl F_(2)N_(6)O_(2)) is of monoclinic system,space group P2_(1)/c with a=10.9998(18),b=18.517(3),c=13.6355(16)?andβ=123.315(9)°.The bioassay results showed all of the target compounds exhibited potential antiproliferative activities against MKN-45,HT-29,A549,K562 and GIST882 cell lines.Among them,compounds 5a,5c and 5e exhibited remarkable inhibitory activities against GIST882,K562 and A549 cell lines with IC_(50 )values of 0.68,0.38 and 0.60μM,respectively,which were comparable to that of the positive control foretinib.