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Synthesis and biological evaluation of vitamin K derivatives as angiogenesis inhibitor
Authors:Tomoko Kayashima  Masaharu Mori  Ryo Mizutani  Kazuyuki Nishio  Kouji Kuramochi  Kazunori Tsubaki  Hiromi Yoshida  Yoshiyuki Mizushina  Kiminori Matsubara
Institution:1. Department of Human Life Science Education, Graduate School of Education, Hiroshima University, 1-1-1 Kagamiyama, Higashi-Hiroshima, Hiroshima 739-8524, Japan;2. Department of Nursing, Faculty of Health and Welfare Science, Okayama Prefectural University, 111 Kuboki, Soja, Okayama 719-1197, Japan;3. Graduate School of Life and Environmental Science, Kyoto Prefectural University, Hangi-cho 1-5, Simogamo, Sakyou-ku, Kyoto 606-8522, Japan;4. Cooperative Research Center of Life Sciences, Kobe-Gakuin University, Chuo-ku, Kobe, Hyogo 651-8586, Japan;5. Laboratory of Food and Nutritional Sciences, Department of Nutritional Science, Kobe-Gakuin University, Nishi-ku, Kobe, Hyogo 651-2180, Japan
Abstract:Ten vitamin K3 derivatives were synthesized and screened for anti-angiogenic activity. Results indicated that amine derivatives (1ad) exerted a stronger inhibition effect on angiogenesis compared to alkyl derivatives (2ad). 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.
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