Synthesis and biological evaluation of vitamin K derivatives as angiogenesis inhibitor.
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.
Kayashima
Tomoko
T
Department of Human Life Science Education, Graduate School of Education, Hiroshima University, 1-1-1 Kagamiyama, Higashi-Hiroshima, Hiroshima 739-8524, Japan. tkaya@shujitsu.ac.jp
Mori
Masaharu
M
Mizutani
Ryo
R
Nishio
Kazuyuki
K
Kuramochi
Kouji
K
Tsubaki
Kazunori
K
Yoshida
Hiromi
H
Mizushina
Yoshiyuki
Y
Matsubara
Kiminori
K
D020533:Angiogenesis Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D000818:Animals; D001011:Aorta / Q000166:cytology / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects; D002478:Cells, Cultured; D042783:Endothelial Cells / Q000187:drug effects; D006801:Humans; D008297:Male; D051381:Rats; D017208:Rats, Wistar; D024483:Vitamin K 3 / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology*
D020533:Angiogenesis Inhibitors; D024483:Vitamin K 3