Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1368499 | Bioorganic & Medicinal Chemistry Letters | 2016 | 4 Pages |
Abstract
In an effort to identify an HIV-1 capsid assembly inhibitor with improved solubility and potency, we synthesized two series of pyrimidine analogues based on our earlier lead compound N-(4-(ethoxycarbonyl)phenyl)-2-(pyridine-4-yl)quinazoline-4-amine. In vitro binding experiments showed that our series of 2-pyridine-4-ylpyrimidines had IC50 values higher than 28 μM. Our series of 2-pyridine-3-ylpyrimidines exhibited IC50 values ranging from 3 to 60 μM. The congeners with a fluoro substituent introduced at the 4-N-phenyl moiety, along with a methyl at C-6, represent potent HIV capsid assembly inhibitors binding to the C-terminal domain of the capsid protein.
Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Milan Kožíšek, Ondřej Štěpánek, Kamil Parkan, Carlos Berenguer Albiñana, Marcela Pávová, Jan Weber, Hans-Georg Krӓusslich, Jan Konvalinka, Aleš Machara,