Synthesis and biological evaluation of vitamin K derivatives as angiogenesis inhibitor.
Synthesis and biological evaluation of vitamin K derivatives as angiogenesis inhibitor.
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DOI：
10.1016/j.bmc.2010.07.022
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发表时间：
2010-09
影响因子：
3.5
通讯作者：
Tomoko Kayashima;Masaharu Mori;Ryoko Mizutani;Kazuyuki Nishio;Kouji Kuramochi;K. Tsubaki;H. Yoshida;Y. Mizushina;K. Matsubara
中科院分区：
文献类型：
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作者：
Tomoko Kayashima;Masaharu Mori;Ryoko Mizutani;Kazuyuki Nishio;Kouji Kuramochi;K. Tsubaki;H. Yoshida;Y. Mizushina;K. Matsubara
合成并筛选了十种维生素 K3 衍生物的抗血管生成活性。结果表明，与烷基衍生物（2a-d）相比，胺衍生物（1a-d）对血管生成具有更强的抑制作用。除了是最有效的抑制剂之外，1b 还抑制人脐静脉内皮细胞管的形成和增殖。这些结果表明，具有较短烷基链的维生素 K3 胺衍生物（例如 1b）可用于开发抗血管生成剂。
Ten vitamin K3derivatives 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 K3amine derivatives with shorter alkyl chains, such as 1b, could be useful for developing anti-angiogenic agents.