Preparation of thienoquinolines for inhibiting KSP kinesin activity.

Abstract

The title compds. I [Y = (un)substituted 5-6 membered (hetero)eryl fused; W = N, CR12; X = N or N-oxide; Z = S, SO, SO2; R1 = H, alkyl, alkoxy, etc.; R3 = H, halo, alkyl, (hetero)aryl, etc.; R12 = H, halo, alkyl, etc.], useful for treating cellular proliferative diseases or disorders assocd. with KSP kinesin activity and for inhibiting KSP kinesin activity, were prepd. E.g., a 2-step synthesis of II, starting from 3-amino-6-tert-butyl-5,6,7,8-tetrahydrothieno[2,3-b]quinoline-2-carbonitrile, was given. II showed IC50 of 0.16 μM when tested for KSP inhibitory activity. The present invention also provides compns. comprising the compds. I. [on SciFinder(R)]