Design and synthesis of a series of novel bisquinazoline glycosides as epidermal growth factor receptor inhibitors.

A new series of potential epidermal growth factor receptor inhibitors possessing bisquinazoline and saccharide moieties were designed and synthesized. The biological results demonstrated that the synthetic derivatives significantly inhibited epidermal growth factor receptor enzymatic activity in vitro. Of them, compound 14b showed the highest inhibitory rate toward epidermal growth factor receptor protein tyrosine kinase (81.36%) at a concentration of 1 μM. Further molecular simulation predicted that 14b offered its saccharide moieties hydrogen bonding to ATP-binding pocket.