Identification of a novel antiangiogenic agent; 4-(N-imidazol-2-ylmethyl)amino benzopyran analogues.
Kim N, Lee S, Yi KY, Yoo SE, Kim G, Lee CO, Park SH, Lee BH.
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.