DESIGN, SYNTHESIS, BIOLOGICAL EVALUATION AND MOLECULAR MODELING STUDY OF NEW BENZOFURAN DERIVATIVES AS POTENTIAL VEGFR2 KINASE INHIBITORS
Mennat Allah Sherifa, Samar S. Tawfik b, Laila A. Abou-Zeida,b*, Fatma El-Nabawia Goda b
a Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Delta university for Science and Technology , Egypt.
b Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Mansoura University, Egypt.
Benzofuran drugs have been reported to have antibiofilm, antioxidants, antidiabetic and anti-inflammatory properties. However, it is debatable whether this pharmacophore nucleus is able to show anticancer properties. Thus, this study aimed to evaluate the potential application of benzofuran as anticancer drugs. For this purpose, a new series of benzofuran containing compounds were designed, synthesized and evaluated biologically for their invitro antitumor activity. Compounds 7 and 9 showed the strongest cytotoxic activity against four tumor cell lines (HePG-2, HCT-116, MCF-7 and PC3) with IC50 range between 7.65-17.92 µg/ml. Molecular modelling studies have been performed for the investigated compounds to evaluate their recognition profiles at the VEGFR active binding-pocket.