The aminoacetylenicoxyquinazoline were synthesized and their structures were confirmed through Infra-Red (IR), Proton Nuclear Magnetic Resonance (1H-NMR), Carbon-13 Nuclear Magnetic Resonance (13C-NMR) and elemental analysis. Docking with Epidural Growth Factor Receptor (EGFR) kinase were carried out and showed effective overlap. The aminoacetylenicoxyquinazoline were tested for their antitumor activities using breast (MCF) and colon (CaCO-2) cancer cell lines. All synthesized compounds exhibited antiproliferative activity but it was weaker than the well-known standard Doxorubicin. Further structural modifications are needed to enhance their antiproliferative effects.