Quinoline derivatives as MELK inhibitors and their preparation and use in the treatment of cancer.

Abstract

The invention directs a compd. represented by formula I that are useful as MELK inhibitors. Compds. of formula I wherein R1 is H, halo, CN, (un)substituted C3-10 cycloalkyl, etc.; R2 is H, halo, OH, (un)substituted aryl, etc.; R3 is H, halo, (un)substituted C1-6 alkyl, C1-6 alkoxy, etc.; R4 is H, halo, CN, etc.; R is H and halo; R101 is H and C1-6 alkyl; and pharmaceutically acceptable salts thereof, are claimed. Example compd. II was prepd. by a multistep procedure (procedure given). All the invention compds. were evaluated for their MELK inhibitory activity. From the assay, it was detd. that compd. II exhibited IC50 value of 0.021 μM. [on SciFinder(R)]