Synthesis and biological evaluation of vitamin K derivatives as angiogenesis inhibitor
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- 作者：Tomoko Kayashima ; Masaharu Mori ; Ryo Mizutani ; Kazuyuki Nishio ; Kouji Kuramochi ; Kazunori Tsubaki ; Hiromi Yoshida ; Yoshiyuki Mizushina ; Kiminori Matsubara
- 关键词：Vitamin K ; 1 ; 4-Naphthoquinone ; Angiogenesis ; Endothelial cells ; Aortic rings
- 刊名：Bioorganic and Medicinal Chemistry
- 出版年：2010
- 出版时间：1 September 2010
- 年：2010
- 卷：18
- 期：17
- 页码：6305-6309
- 全文大小：345 K
文摘
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.