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The Halogen Bond.卤键
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J Med Chem. 2015 Nov 12;58(21):8315-59. doi: 10.1021/acs.jmedchem.5b00258. Epub 2015 Jul 22.
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丙烯酰胺官能团的引入改善类药物性质：以表皮生长因子受体抑制剂为例

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

作者信息

Wu Kuen-Da, Chen Grace Shiahuy, Liu Jia-Rong, Hsieh Chen-En, Chern Ji-Wang

机构信息

School of Pharmacy and Center for Innovative Therapeutics Discovery, National Taiwan University, Taipei 10055, Taiwan.

Department of Applied Chemistry, Providence University, Taichung 43301, Taiwan.

出版信息

ACS Med Chem Lett. 2018 Dec 6;10(1):22-26. doi: 10.1021/acsmedchemlett.8b00270. eCollection 2019 Jan 10.

DOI:10.1021/acsmedchemlett.8b00270
PMID:30655941
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6331160/
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 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.

摘要

我们证明，丙烯酰胺基团可用于改善潜在药物候选物的类药性质。在表皮生长因子受体（EGFR）抑制剂的研发中，分别含有一个丙烯酰胺基团的化合物 和 的溶解性及膜通透性均显著优于吉非替尼（ ）和AZD3759（ ）。我们证明，引入丙烯酰胺部分可作为改善类药性质的良好策略。