Synthesis and biological evaluation of vitamin K derivatives as angiogenesis inhibitor

Abstract Ten vitamin K 3 derivatives were synthesized and screened for anti-angiogenic activity. Results indicated that amine derivatives ( 1a – d ) exerted a stronger inhibition effect on angiogenesis compared to alkyl derivatives ( 2a – d ). In addition to being the most potent inhibitor, 1b also suppressed human umbilical vein endothelial cell tube formation and proliferation. These results suggest that vitamin K 3 amine derivatives with shorter alkyl chains, such as 1b , could be useful for developing anti-angiogenic agents.