Pyrimido-oxazepine as a versatile template for the development of inhibitors of specific kinases

Weitao Pan; Hu Liu; Yong-Jiang Xu; Xin Chen; Ki Hwan Kim; Daniel L Milligan; John Columbus; Yaron R Hadari; Paul Kussie; Wai C Wong; Marc Labelle

doi:10.1016/j.bmcl.2005.08.098

Pyrimido-oxazepine as a versatile template for the development of inhibitors of specific kinases

Bioorg Med Chem Lett. 2005 Dec 15;15(24):5474-7. doi: 10.1016/j.bmcl.2005.08.098. Epub 2005 Sep 28.

Authors

Weitao Pan¹, Hu Liu, Yong-Jiang Xu, Xin Chen, Ki Hwan Kim, Daniel L Milligan, John Columbus, Yaron R Hadari, Paul Kussie, Wai C Wong, Marc Labelle

Affiliation

¹ Department of Chemistry, ImClone Systems Incorporated, 710 Parkside Avenue, Brooklyn, NY 11226, USA.

PMID: 16198560
DOI: 10.1016/j.bmcl.2005.08.098

Abstract

Pyrimido-oxazepine based sub-micromolar inhibitors (2-4) for Aurora and FLT-3 were designed and synthesized. These preliminary results supported the potential use of pyrimido-oxazepines as a versatile template for developing specific kinase inhibitors.

MeSH terms

Aurora Kinases
Enzyme Inhibitors / chemical synthesis*
Enzyme Inhibitors / pharmacology*
Humans
Kinetics
Models, Molecular
Oxazepines / chemical synthesis
Oxazepines / pharmacology*
Phosphotransferases / antagonists & inhibitors*
Protein Serine-Threonine Kinases / antagonists & inhibitors
Pyrimidines / chemical synthesis
Pyrimidines / pharmacology*
Structure-Activity Relationship
fms-Like Tyrosine Kinase 3 / antagonists & inhibitors

Substances

Enzyme Inhibitors
Oxazepines
Pyrimidines
Phosphotransferases
FLT3 protein, human
fms-Like Tyrosine Kinase 3
Aurora Kinases
Protein Serine-Threonine Kinases