Synthesis, discovery and preliminary SAR study of benzofuran derivatives as angiogenesis inhibitors.
A series of benzofuran derivatives were synthesized and evaluated against HUVEC proliferation. Among these compounds, compound 32 exhibited good inhibitory activity and remarkable selectivity to HUVEC. Our current data suggested that array order of methyl, acrylate and carboxylate groups in benzofuran scaffold is the basic requirement for inhibitory activity against HUVEC proliferation. These results demonstrated that benzofuran scaffold represents a promising structural core to discover a new class of active and selective angiogenesis inhibitors.
Chen
Yuan
Y
Guangzhou Institute of Biomedicine and Health, Chinese Academy of Sciences, Guangzhou, Guangdong 510663, PR China.
Chen
Shaopeng
S
Lu
Xin
X
Cheng
Hao
H
Ou
Yingyong
Y
Cheng
Huimin
H
Zhou
Guo-Chun
GC
D000179:Acrylates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D020533:Angiogenesis Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001572:Benzofurans / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D049109:Cell Proliferation; D055808:Drug Discovery; D006801:Humans; D020128:Inhibitory Concentration 50; D013329:Structure-Activity Relationship
D000179:Acrylates; D020533:Angiogenesis Inhibitors; D001572:Benzofurans