A diaminocyclohexyl analog of SNS-032 with improved permeability and bioavailability properties.
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.
Choong
Ingrid C
IC
Medicinal Chemistry, Sunesis Pharmaceuticals, South San Francisco, CA 94080, USA. ichoong2@gmail.com
Serafimova
Iana
I
Fan
Junfa
J
Stockett
David
D
Chan
Erica
E
Cheeti
Sravanthi
S
Lu
Yafan
Y
Fahr
Bruce
B
Pham
Phuongly
P
Arkin
Michelle R
MR
Walker
Duncan H
DH
Hoch
Ute
U
D000818:Animals; D001682:Biological Availability; D051379:Mice; D010080:Oxazoles / Q000737:chemistry* / Q000493:pharmacokinetics*; D010539:Permeability; D013844:Thiazoles / Q000737:chemistry* / Q000493:pharmacokinetics*
C484864:N-(5-(((5-(1,1-dimethylethyl)-2-oxazolyl)methyl)thio)-2-thiazolyl)-4-piperidinecarboxamide; D010080:Oxazoles; D013844:Thiazoles