| Autor: |
Christian M. Martin, Jennifer Proctor, Patrick O'Hearn, Janid A. Ali, Andre Lescarbeau, Jennifer Hoyt, Jonathan P. DiNitto, Ann M. Rowley, Thomas T. Tibbitts, Catherine A. Evans, Martin R. Tremblay, Tao Liu, Vito J. Palombella, John Soglia, Johan A. Pradeilles, Somarajan J. Nair, Melissa Pink, David G. Winkler, Stanley Goldstein, Quentin Glenadel, Erin L. O’Hearn, Culver Cheung, Erin Brophy, Alfredo C. Castro, Louis Grenier |
| Rok vydání: |
2016 |
| Předmět: |
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| Zdroj: |
ACS Medicinal Chemistry Letters. 7:862-867 |
| ISSN: |
1948-5875 |
| DOI: |
10.1021/acsmedchemlett.6b00238 |
| Popis: |
Optimization of isoquinolinone PI3K inhibitors led to the discovery of a potent inhibitor of PI3K-γ (26 or IPI-549) with >100-fold selectivity over other lipid and protein kinases. IPI-549 demonstrates favorable pharmacokinetic properties and robust inhibition of PI3K-γ mediated neutrophil migration in vivo and is currently in Phase 1 clinical evaluation in subjects with advanced solid tumors. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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