A diaminocyclohexyl analog of SNS-032 with improved permeability and bioavailability properties

Ingrid C Choong; Iana Serafimova; Junfa Fan; David Stockett; Erica Chan; Sravanthi Cheeti; Yafan Lu; Bruce Fahr; Phuongly Pham; Michelle R Arkin; Duncan H Walker; Ute Hoch

doi:10.1016/j.bmcl.2008.09.073

A diaminocyclohexyl analog of SNS-032 with improved permeability and bioavailability properties

Bioorg Med Chem Lett. 2008 Nov 1;18(21):5763-5. doi: 10.1016/j.bmcl.2008.09.073. Epub 2008 Sep 24.

Authors

Ingrid C Choong¹, Iana Serafimova, Junfa Fan, David Stockett, Erica Chan, Sravanthi Cheeti, Yafan Lu, Bruce Fahr, Phuongly Pham, Michelle R Arkin, Duncan H Walker, Ute Hoch

Affiliation

¹ Medicinal Chemistry, Sunesis Pharmaceuticals, South San Francisco, CA 94080, USA. [email protected]

PMID: 18842409
DOI: 10.1016/j.bmcl.2008.09.073

Abstract

The identification of a selective CDK2, 7, 9 inhibitor 4 with improved permeability is described. Compound 4 exhibits comparable CDK selectivity profile to SNS-032, but shows improved permeability and higher bioavailability in mice.

MeSH terms

Animals
Biological Availability
Mice
Oxazoles / chemistry*
Oxazoles / pharmacokinetics*
Permeability
Thiazoles / chemistry*
Thiazoles / pharmacokinetics*

Substances

N-(5-(((5-(1,1-dimethylethyl)-2-oxazolyl)methyl)thio)-2-thiazolyl)-4-piperidinecarboxamide
Oxazoles
Thiazoles