Abstract
A series of 2-methyl-5-nitrobenzenesulfonohydrazides were prepared and evaluated as inhibitors of PI3K. An isoquinoline derivative shows good selectivity for the p110alpha isoform over p110beta and p110delta, and also demonstrates good in vitro activity in a cell proliferation assay. Molecular modelling provides a rationalisation for the observed SAR.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Amino Acid Sequence
-
Androstadienes / pharmacology
-
Cell Line
-
Cell Proliferation / drug effects
-
Chromones / pharmacology
-
Drug Evaluation
-
Enzyme Inhibitors / chemical synthesis*
-
Enzyme Inhibitors / chemistry
-
Enzyme Inhibitors / pharmacology*
-
Hydrazines / chemistry*
-
Hydrazines / pharmacology
-
Models, Molecular
-
Molecular Sequence Data
-
Morpholines / pharmacology
-
Nitrobenzenes / chemistry*
-
Nitrobenzenes / pharmacology
-
Phosphoinositide-3 Kinase Inhibitors*
-
Protein Kinase Inhibitors / pharmacology
-
Sequence Alignment
-
Structure-Activity Relationship
-
Wortmannin
Substances
-
2-methyl-5-nitrobenzenesulfonohydrazide
-
Androstadienes
-
Chromones
-
Enzyme Inhibitors
-
Hydrazines
-
Morpholines
-
Nitrobenzenes
-
Phosphoinositide-3 Kinase Inhibitors
-
Protein Kinase Inhibitors
-
2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one
-
Wortmannin