New phthalazine derivatives as vascular endothelial growth factor receptor-2 (VEGFR-2) inhibitors were synthesized joined to different spacers including pyrazole, α,β-unsaturated ketonic fragment, pyrimidinone and/or pyrimidinthione.
Essential structural motifs for design of Lead against VEGFR-2.
The review describes anti-VEGFR-2 activity of heterocycles including quinazoles, pyrimidines, isatin and azoles considering SAR for a given set of derivatives. Compounds with potent activity were emphasized with description of structural features.
A novel series of quinazoline-based compounds were designed and synthesized as modified analogues to certain known VEGFR-2 inhibitors, as an extension of our work on the design and synthesis of new VEGFR-2 inhibitors.
Design, synthesis and in vitro and in silico studies of novel quinoxaline-based derivatives as antitumor VEGFR-2 inhibitors with apoptotic activities.