INDEX
Page
Preface
……… 1Introduction
………..…. 5Tyrosine Kinase Receptors (RTKs)……… 5
Design of Tyrosine Kinase Inhibitors………... 7
Indirect and Direct Targeting of Angiogenesis Pathways……… 10
Vascular Endothelial Growth Factor and Receptors VEGF/VEGFR… 11 VEGFR signalling………. 13
VEGF/VEGFR in angiogenesis……….. 15
Anti-VEGFR Agents………. 16
Monoclonal Antibody……… 17
Small molecules TK Inhibitors……… 18
Introduction to Experimental Section
………. 22VEGFR-2 small molecules Inhibitors………... 22
Anthranilamides……… 23
Pyrimidine Derivatives……….. 25
New Benzothiopyrano and Pyridothiopyrano Pyrimidines……….. 31
Chemical synthesis of the 2-aryl substituted benzothiopyrano-pyrimidines……… 37
Chemical synthesis of the 2-aryl substituted pyridothiopyrano-pyrimidines……... 40