Design, synthesis and in vitro antitumor activity of novel phthalazin-1,4- dione/chalcone hybrids and phthalazin-1,4-dione/pyrazoline hybrids

Said A.H. El-Feky, Hanan A. Ab

Abstract

In continuation of our study of phthalazinones with antitumor activity, several new phthalazin-1,4-diones based on the structure of vatalanib (PTK787) were designed and synthesized. The cytotoxicity of the final compounds was tested in vitro on HCT-116 colon cancer and MCF-7 breast cancer. Compound 4f exerted the highest cytotoxic activity against both colon cancer and breast cancer with IC50values equal to 2.21and 1.0μΜ respectively. Besides, 4f demonstrated the highest binding profiles into VEGF-2 generated by MOE docking.