2. Academic Validation
  3. Acrylamide Functional Group Incorporation Improves Drug-like Properties: An Example with EGFR Inhibitors

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

  • ACS Med Chem Lett. 2018 Dec 6;10(1):22-26. doi: 10.1021/acsmedchemlett.8b00270.
Kuen-Da Wu 1,  Grace Shiahuy Chen 2,  Jia-Rong Liu 1,  Chen-En Hsieh 2,  Ji-Wang Chern 1
Affiliations

Affiliations

  • 1 School of Pharmacy and Center for Innovative Therapeutics Discovery, National Taiwan University, Taipei 10055, Taiwan.
  • 2 Department of Applied Chemistry, Providence University, Taichung 43301, Taiwan.
PMID: 30655941 DOI: 10.1021/acsmedchemlett.8b00270
Abstract

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.

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