Identification of a novel antiangiogenic agent; 4-(N-imidazol-2-ylmethyl)amino benzopyran analogues.
A series of 4-(N-imidazol-2-ylmethyl)aminobenzopyran analogues, originally designed as K(ATP) openers for ischemic diseases, showed antiangiogenic properties through the inhibition of HUVEC tube formation. Especially one of p-Cl substituted analogues (4c) completely inhibited HUVEC tube formation at 10 microM. The compound 4c significantly inhibited tumor growth by 52% on A549 (human non small cell lung carcinoma) in nude mice xenografts without any significant side effects.
Department of Chemistry, Chungnam National University, Taejon 305-764, South Korea.
Nakjeong
N
Kim
Sunkyung
S
Lee
Kyu Yang
KY
Yi
Sung-eun
SE
Yoo
Guncheol
G
Kim
Chong Ock
CO
Lee
Sung Hee
SH
Park
Byung Ho
BH
Lee
D020533:Angiogenesis Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology / Q000633:toxicity; D045744:Cell Line, Tumor; D042783:Endothelial Cells / Q000187:drug effects; D006801:Humans; D051379:Mice; D008819:Mice, Nude; D009374:Neoplasms, Experimental / Q000150:complications / Q000188:drug therapy; D013329:Structure-Activity Relationship; D014183:Transplantation, Heterologous; D016896:Treatment Outcome; D014471:Umbilical Veins / Q000166:cytology
D020533:Angiogenesis Inhibitors; D000970:Antineoplastic Agents