Previous research within our laboratories identified the 3-hydroxypyrrolidine scaffold 1 as a new and selectiveintegrin α5β1 inhibitor class which was designed for local administration. Herein the discovery of new orallyavailableintegrin α5β1 inhibitor scaffolds for potential systemic treatment is described.
The present invention provides novel compounds that are antagonists of PI3 kinase, PI3 kinase and tryosine kinase, PI3Kinase and mTOR, or PI3Kinase, mTOR and tryosine kinase.
Synthesis of a 2(1<i>H</i>)-Pyridone Library via Rhodium-Catalyzed Formation of Isomunchones
作者:Subhasis De、Lu Chen、Shuxing Zhang、Scott R. Gilbertson
DOI:10.1021/co400067q
日期:2013.7.8
Through the use of the dipolar cycloaddition of isomunchones with olefins the 2(1H)-pyridone ring system has been synthesized.(1) The use of different cyclization partners followed by diversification of the initial scaffold has provded libraries of 4-hydroxy-2(1H)-pyridones. There are no examples of this ring system in either PubChem or the MLSMR