Zobrazeno 1 - 4
of 4
pro vyhledávání: '"Leonard D. Rodman"'
Autor:
John T. Sisko, Christine Fernandes, Bradley K. Wong, Patrice A. Ciecko, Nancy E. Kohl, Mark T. Bilodeau, Keith W. Rickert, Laura Sepp-Lorenzino, Leonard D. Rodman, Timothy J. Koester, Jackson B. Gibbs, Cynthia Miller-Stein, Debra A. McLoughlin, Joseph J. Lynch, Carolyn A. Buser, George D. Hartman, Xianzhi Mao, Kathleen E. Coll, Kenneth A. Thomas, Jennifer M. Shipman, Thomas J. Tucker
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:1146-1150
Pyrimidino-thiazolyl carbonitriles were prepared that are potent VEGFR-2 (KDR) kinase inhibitors. The modification of lead structures resulted in 3m which exhibited the best overall profile in KDR inhibitory activity, iv/po pharmacokinetics, and redu
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::84e8b7d13a4632a1e8e93688c9eb9ed9
https://doi.org/10.1016/j.bmcl.2005.11.089
https://doi.org/10.1016/j.bmcl.2005.11.089
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7803b8fb364a80f776c25f0422cd590b
https://doi.org/10.1021/jm049697f
https://doi.org/10.1021/jm049697f
Autor:
Hungate Randall W, Timothy J. Koester, William F. Hoffman, Keith W. Rickert, Kathleen E. Coll, Georgia B. McGaughey, Kenneth A. Thomas, Leonard D. Rodman, Richard L. Kendall, Mark T. Bilodeau, Rosemary C. McFall, Ruth Z. Rutledge
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:2941-2945
An azo-dye lead was modified to a novel N-(1,3-thiazol-2-yl)pyridin-2-amine series of KDR kinase inhibitors through the use of rapid analog libraries. This new class has been found to be potent, selective, and of low molecular weight. Molecular model
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::610da51c8d1f557021fd3a6ce01f2efa
https://doi.org/10.1016/j.bmcl.2004.03.052
https://doi.org/10.1016/j.bmcl.2004.03.052
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::021d1bb9daf7639be702b1e7ab112c01
https://doi.org/10.1016/s0960-894x(03)00244-0
https://doi.org/10.1016/s0960-894x(03)00244-0