| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1364150 | Bioorganic & Medicinal Chemistry Letters | 2009 | 5 Pages |
Abstract
A homology model of the p110α catalytic subunit of PI3Kα was generated from the p110γ crystal structure. Using this model, an isonicotinic scaffold was designed for chemically exploring the PI3Kα and γ binding sites. A focused library of derivatives was synthesized and tested. The morpholine acids 5a and 5b proved to be the most potent analogs.
Graphical abstractUsing a homology model of PI3Kα based of PI3Kγ, a series of isonicotinic acid derivatives was designed and synthesized for studying the PI3Kα and γ active sites.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Philip T. Cherian, Leonid N. Koikov, Matthew D. Wortman, James J. Knittel,