The invention discloses a 5,8-disubstituted-1,6-quinazoline-7-amidocarbonylation compound, a preparing method, an application and a drug composite containing the compound thereof. More specifically, the invention discloses a 5,8-disubstituted-1,6-quinazoline-7-amidocarbonylation compound as shown in the formula I, a preparing method and an application thereof. By the growth inhibition test of various tumour cell lines (human breast cancer cells MDA-MB-435, p53-deleted poorly differentiated colorectal adenocarcinoma cells Hct116p53-/-, p53-enriched poorly differentiated colorectal adenocarcinoma cells Hct116p53+/+, human breast cancer cells Mcf-7, NIH189, human breast cancer cells SkBr-3, prostatic cancer cells LnCap, LnHer, human colorectal cancer cells HT29 and human ovarian cancer cellsHEY), the compound has favourable inhibition activity for the above tumour cells and can treat diseases caused by tumour cell malignant proliferation. The invention also discloses a drug composite containing the compound.