| abstract |
The invention relates to a 2,4-dinitrogen-containing group-substituted pyrimidine compound, a preparation method and application thereof, and belongs to the technical field of medicinal chemistry. This class of 2,4-dinitrogen-containing group-substituted pyrimidine compounds with the structural characteristics of general formula I can selectively inhibit the activity of mutant epithelial growth factor receptor (EGFR), including single point mutation T790M and double point mutations such as L858R/T790M, ex19del/T790M. At the same time, it also has inhibitory activity against EGFR single-point activating mutations such as L858R and ex19del. Such compounds have weak inhibitory effect on wild-type EGFR and have very high selectivity. It has the potential to be used as a drug for the treatment of malignant tumors with EGFR mutation, especially non-small cell lung cancer (NSCLC) carrying T790M EGFR mutation, and has great application value. |