Synthesis and biological evaluation of vitamin K derivatives as angiogenesis inhibitor

Ten vitamin K3 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 K3 amine derivatives with shorter alkyl chains, such as 1b, could be useful for developing anti-angiogenic agents.

Among the vitamin K derivatives synthesized, 1b showed the strongest anti-angiogenic effect under both ex vivo and in vitro conditions. Longer alkyl chains weaken anti-angiogenic activity.Figure optionsDownload as PowerPoint slide