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

• 作者: LIU Ju WU Shuang WANG Huan DU Si-Yuan LI Zhen SHEN Ji-Wei CHEN Ye DING Shi
• 来源期刊: 结构化学
• 年，卷（期）: 2022,（2）
• 所属期刊栏目: organic and inorganic structural chemistry
• 页码范围: 132-140
• 页数: 9页
• 语种: 英文
• DOI: 10.14102/j.cnki.0254-5861.2011-3283

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 (C25H20ClFN6O2) belongs to the monoclinic system,space group P21/c with a =11.0500(10),b =18.3045(17),c =13.5646(9) (A) and β =122.806(5)°.5e (C25H19ClF2N6O2) is of monoclinic system,space group P21/c with a =10.9998(18),b =18.517(3),c =13.6355(16) (A) 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 IC50 values of 0.68,0.38 and 0.60 μM,respectively,which were comparable to that of the positive control foretinib.