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

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 tha...

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Veröffentlicht in:	ACS medicinal chemistry letters 2019-01, Vol.10 (1), p.22-26
Hauptverfasser:	Wu, Kuen-Da, Chen, Grace Shiahuy, Liu, Jia-Rong, Hsieh, Chen-En, Chern, Ji-Wang
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Sprache:	eng
Schlagworte:	Letter
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creator	Wu, Kuen-Da Chen, Grace Shiahuy Liu, Jia-Rong Hsieh, Chen-En Chern, Ji-Wang
description	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.
doi_str_mv	10.1021/acsmedchemlett.8b00270
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title	Acrylamide Functional Group Incorporation Improves Drug-like Properties: An Example with EGFR Inhibitors
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