Topological designing of 4-piperazinylquinazolines as antagonists of PDGFR tyrosine kinase family.
Topological designing of a series of 4-piperazinylquinazolines as antagonists of platelet-derived growth factor receptor (PDGFR) tyrosine kinase family has been reported using a series of distance-based topological indices. Regression analysis of the data, using maximum R(2) method indicated that inhibitory activity, pIC(50) (microm), in cellular PGDFR phosphorylation assay can be modelled excellently in multi-parametric model. The results are discussed critically using cross-validated parameters.
Khadikar
Padmakar V
PV
Research Division, Laxmi Fumigation and Pest Control Pvt. Ltd., 3 Khatipura, Indore-452 007, India. pvkhadikar@rediffmail.com
Shrivastava
Anjali
A
Agrawal
Vijay K
VK
Srivastava
Shachi
S
D000818:Animals; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D020128:Inhibitory Concentration 50; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors; D021281:Quantitative Structure-Activity Relationship; D011799:Quinazolines / Q000737:chemistry* / Q000494:pharmacology; D017479:Receptors, Platelet-Derived Growth Factor / Q000037:antagonists & inhibitors*; D012044:Regression Analysis
D004791:Enzyme Inhibitors; D011799:Quinazolines; D011505:Protein-Tyrosine Kinases; D017479:Receptors, Platelet-Derived Growth Factor