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• 26 new quinazolin based antiproliferative and antiangiogenic agents are synthesized. • The proliferation rate of PC3 cells was reduced by 9f (IC 50 = 17.7 μ M) vs sorafenib (17.3 μ M). • CAM assay revealed that the growth of blood vessels was inhibited by 9f moderately. • Western blot analysis of 9f revealed the inhibition of VEGFR-2 phosphorylation. A series of quinazolin-4(3 H)-one based agents containing thiadiazole-urea were designed, synthesized, and biologically evaluated. The proliferation rate of PC3 cells was moderately reduced by compound 9f (IC 50 = 17.7 μ M) which was comparable with sorafenib (IC 50 = 17.3 μ M). There was also a significant reduction in the number of HUVEC cells, when they were exposed to compound 9y (IC 50 = 6.1 μ M). To test the potential of compounds in inducing apoptosis, Annexin V-FITC/propidium iodide double staining assay was used. After the treatment of HUVEC cells with 9f , they underwent apoptotic effects. A substantial effort was dedicated to gathering comprehensive data across CAM assay. These data showed that 9f moderately inhibits the growth of corresponding blood vessels. Finally, the outcomes of Western blotting proposed a mechanism of action, by which the phosphorylation of VEGFR-2 is inhibited by compounds 9f and 9y. [ABSTRACT FROM AUTHOR]