Zobrazeno 1 - 4
of 4
pro vyhledávání: '"Adrienne E. Balitza"'
Autor:
Keith W. Rickert, Christine Fernandes, Xianzhi Mao, Kathleen E. Coll, George D. Hartman, Bradley K. Wong, Peter J. Manley, Adrienne E. Balitza, Timothy J. Koester, Mark T. Bilodeau, Debra A. McLoughlin, David C. Heimbrook, Rosemary C. McFall, Sean Yu, William R. Huckle, Jackson B. Gibbs, Jennifer M. Shipman, Kenneth A. Thomas, Raju Subramanian, Joseph J. Lynch, Nancy E. Kohl, Leonard D. Rodman, Cynthia Miller-Stein, Laura Sepp-Lorenzino, Carolyn Buser-Doepner
Publikováno v:
Journal of Medicinal Chemistry. 47:6363-6372
A series of N-(1,3-thiazol-2-yl)pyridin-2-amine KDR kinase inhibitors have been developed that possess optimal properties. Compounds have been discovered that exhibit excellent in vivo potency. The particular challenges of overcoming hERG binding act
Autor:
George D. Hartman, Kenneth A. Thomas, Mark T. Bilodeau, Kathleen E. Coll, Keith W. Rickert, Leonard D. Rodman, Adrienne E. Balitza, Rosemary C. McFall, Peter J. Manley
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:1673-1677
2,4-Disubstituted pyrimidines were synthesized as a novel class of KDR kinase inhibitors. Evaluation of the SAR of the screening lead compound 1 (KDR IC(50)=105 nM, Cell IC(50)=8% inhibition at 500 nM) led to the potent 3,5-dimethylaniline derivative
Autor:
Deborah Defeo-Jones, Anthony M. Smith, Ronald G. Robinson, Mark T. Bilodeau, Stanley F. Barnett, George D. Hartman, Raymond E. Jones, Karen R. Leander, Jacob M. Hoffman, Peter J. Manley, Adrienne E. Balitza, Kathleen M. Haskell, Hans E. Huber
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(11)
A series of naphthyridine and naphthyridinone allosteric dual inhibitors of Akt1 and 2 have been developed. These compounds have been optimized to have potent dual activity against the activated kinase as well as the activation of Akt in cells. One m
Autor:
Kathleen E. Coll, Jennifer M. Shipman, Zhicai Wu, Keith W. Rickert, Laura Sepp-Lorenzino, Edward S. Tasber, Mark E. Fraley, Bin Shi, Mildred L. Kaufman, Mark T. Bilodeau, Kenneth A. Thomas, Adrienne E. Balitza, George D. Hartman
Publikováno v:
Bioorganicmedicinal chemistry letters. 14(4)
3,7-Diarylsubstituted imidazopyridines were designed and developed as a new class of KDR kinase inhibitors. A variety of imidazopyridines were synthesized and potent inhibitors of KDR kinase activity were identified with good aqueous solubility.