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 and , each containing an acrylamide group, were substantially better than those of gefitinib () and AZD3759 (), respectively. We demonstrated that incorporation of an acrylamide moiety could serve as a good strategy for improving drug-like properties.
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| http://dx.doi.org/10.1021/acsmedchemlett.8b00270 | DOI Listing |
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