Synthesis and anti-angiogenesis activity of coumarin derivatives.
A series of 7-diethylaminocoumarin compounds were synthesized and the cytotoxicities were tested against human umbilical vein endothelial cell (HUVEC) and some cancer cells. We found that the introduction of cyano groups at the 4-position will promote the bioactivity. In particular, compounds 9 and 10 strongly inhibited the proliferation of various cancer cell lines, and 12 and 15 showed a high selectivity for HUVEC. Therefore, these coumarin molecules can be utilized as lead compounds to develop potential nontoxic angiogenesis inhibitors and small molecular ligands to target HUVEC.
Lee
Seokjoon
S
Department of Chemistry and Biochemistry, University of South Carolina, Columbia, 29203, USA. sjlee@kwandong.ac.kr
Sivakumar
Krishnamoorthy
K
Shin
Woon-Seob
WS
Xie
Fang
F
Wang
Qian
Q
D020533:Angiogenesis Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D049109:Cell Proliferation / Q000187:drug effects; D002478:Cells, Cultured; D003374:Coumarins / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology* / Q000633:toxicity; D006801:Humans; D015394:Molecular Structure
D020533:Angiogenesis Inhibitors; D003374:Coumarins; C030123:coumarin