Acrylamide Functional Group Incorporation Improves Drug-like Properties: An Example with EGFR Inhibitors

摘要

We demonstrate that the acrylamide group can be used to improve the drug-like properties of potential drug candidates. In the EGFR inhibitor development, both the solubility and membrane permeability properties of compounds 6a and 7 , each containing an acrylamide group, were substantially better than those of gefitinib (1 ) and AZD3759 (2 ), respectively. We demonstrated that incorporation of an acrylamide moiety could serve as a good strategy for improving drug-like properties.