Department of Human Life Science Education, Graduate School of Education, Hiroshima University, 1-1-1 Kagamiyama, Higashi-Hiroshima, Hiroshima 739-8524, Japan.
Bioorg Med Chem. 2010 Sep 1;18(17):6305-9. doi: 10.1016/j.bmc.2010.07.022. Epub 2010 Jul 13.
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.
合成了 10 种维生素 K(3)衍生物，并对其抗血管生成活性进行了筛选。结果表明，与烷基衍生物（2a-d）相比，胺衍生物（1a-d）对血管生成的抑制作用更强。1b 不仅是最强的抑制剂，还能抑制人脐静脉内皮细胞的管腔形成和增殖。这些结果表明，具有较短烷基链的维生素 K(3)胺衍生物，如 1b，可能有助于开发抗血管生成药物。
