Acrylamide Functional Group Incorporation Improves Drug-like Properties: An Example with EGFR Inhibitors
| Autor: | Chen-En Hsieh, Grace Shiahuy Chen, Ji-Wang Chern, Kuen-Da Wu, Jia-Rong Liu |
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| Rok vydání: | 2018 |
| Předmět: |
Drug
Membrane permeability 010405 organic chemistry media_common.quotation_subject Organic Chemistry 01 natural sciences Biochemistry Combinatorial chemistry 0104 chemical sciences 010404 medicinal & biomolecular chemistry chemistry.chemical_compound Gefitinib chemistry Acrylamide Drug Discovery Lipophilicity medicine Moiety Solubility EGFR inhibitors medicine.drug media_common |
| Zdroj: | ACS Medicinal Chemistry Letters. 10:22-26 |
| ISSN: | 1948-5875 |
| DOI: | 10.1021/acsmedchemlett.8b00270 |
| Popis: | [Image: see text] 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. |
| Databáze: | OpenAIRE |
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