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典型文献
Novel 2,4-Diarylaminopyrimidine Derivatives Containing Pyridine Moiety:Design,Synthesis,Crystal Structure and Biological Evaluation
文献摘要:
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.
文献关键词:
作者姓名:
LIU Ju;WU Shuang;WANG Huan;DU Si-Yuan;LI Zhen;SHEN Ji-Wei;CHEN Ye;DING Shi
作者机构:
College of Pharmacy of Liaoning University,Shenyang 110036,China;API Engineering Technology Research Center of Liaoning Province,Shenyang 110036,China;Small Molecular Targeted Drug R&D Engineering Research Center of Liaoning Province,Shenyang 110036,China
文献出处:
引用格式:
[1]LIU Ju;WU Shuang;WANG Huan;DU Si-Yuan;LI Zhen;SHEN Ji-Wei;CHEN Ye;DING Shi-.Novel 2,4-Diarylaminopyrimidine Derivatives Containing Pyridine Moiety:Design,Synthesis,Crystal Structure and Biological Evaluation)[J].结构化学,2022(02):132-140
A类:
Diarylaminopyrimidine,Moiety,diarylaminopyrimidine,C25H20ClFN6O2,C25H19ClF2N6O2,GIST882,foretinib
B类:
Novel,Derivatives,Containing,Pyridine,Design,Synthesis,Crystal,Structure,Biological,Evaluation,series,derivatives,containing,pyridine,were,designed,synthesized,crystal,structures,compounds,5d,5e,obtained,from,ray,diffraction,belongs,monoclinic,system,space,group,P21,bioassay,results,showed,all,target,exhibited,potential,antiproliferative,activities,against,MKN,HT,A549,K562,cell,lines,Among,them,5a,5c,remarkable,inhibitory,IC50,values,respectively,which,comparable,that,positive,control
AB值:
0.557366
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