Author/Authors :
Mark T. Bilodeau، نويسنده , , April M. Cunningham، نويسنده , , Timothy J. Koester، نويسنده , , Patrice A. Ciecko، نويسنده , , Kathleen E. Coll، نويسنده , , William R. Huckle، نويسنده , , Randall W. Hungate، نويسنده , , Richard L. Kendall، نويسنده , , Rosemary C. McFall، نويسنده , , Xianzhi Mao، نويسنده , , Ruth Z. Rutledge، نويسنده , , Kenneth A. Thomas، نويسنده ,
Abstract :
1,5-Diarylbenzimidazoles have been identified as potent inhibitors of KDR kinase activity. The series was developed with a goal of finding compounds with optimal drug-like properties. This communication describes structural modifications in the series that enhance solubility, lower protein binding, and provide compounds with excellent potency and pharmacokinetic profiles.
