Compounds For Treating Or Preventing Cancer

Exhibitor: NATIONAL DEFENSE MEDICAL CENTER

Booth No: R1122

Characteristic

Target drugs are promising therapeutic target for tumor treatment in recent years, tumor angiogenesis inhibiting is one of most promising pathways for target therapy. The target compounds were obtained by condensation of 5-substituted oxindoles with N-substituted 2-pyrrolidone aldehyde 7 in satisfactory yields. Of these, 11, 12, 23 and 24 had the highest potency and, compared to sunitinib, showed: (1) significant increase in anti-proliferation of various cancer cells with a favorable selective index (SI); (2) higher inhibitory potency against both VEGFR-2 and PDGFRβ. The molecular modeling results showed that, in terms of VEGFR-2 binding, the synthetic products had a similar binding mode to sunitinib but with tighter interaction. The experimental results suggest that 11, 12, 23 and 24 might be promising anti-angiogenesis agents.