Preparation of quinoline derivatives for treating and/or preventing cancer.

Abstract

The invention relates to quinoline derivs. I [wherein X = O or S; Y = H or halo; Z = Ar1-Ar2; n = 2-6; R1 and R2 = independently (un)substituted alkyl, cycloalkyl, alkenyl, or alkynyl; or R1 and R2 together with the attached N to form heterocyclyl; Ar1 and Ar2 = independently aryl or heteroaryl; R4 and R5 = independently H, hydroxyl, halo, nitro, amino, cyano, etc.], pharmaceutically acceptable salts, hydrates, solvates, and prodrugs thereof as c-Met kinase inhibitors for treating and/or preventing cancer. For example, II was prepd. in a multi-step synthesis, which showed inhibitory activity with IC50 of 1.5, 0.54, 0.55, 0.29, and 1.4 mg/mL against HT-29, H460, MKN-45, A549, and U-87 cancer cell lines, resp. [on SciFinder(R)]