Design, synthesis and antitumor activity of novel thiophene-pyrimidine derivatives as EGFR inhibitors overcoming T790M and L858R/T790M mutations
Zhen Xiao, Zhihui Zhou, Cilong Chu, Qian Zhang, Lingjia Zhou, Zunhua Yang, Xin Li, Liying Yu, Pengwu Zheng, Shan Xu, Wufu Zhu
Topics & Concepts
ChemistryT790MCell culturePyrimidineApoptosisThiopheneStructure–activity relationshipCancer cellA549 cellStereochemistryA431 cellsCell growthCancerLead compoundIC50Growth inhibitionBiochemistryCell cycleMutationIn vitroGeneBiologyOncogeneGeneticsKRASOrganic chemistryLung Cancer Treatments and MutationsCancer therapeutics and mechanismsSynthesis and biological activity