Quinazolinone inhibitors of dynein

摘要

Compounds of formula (I) in which R3 is chosen from hydrogen, cyano, nitro, acetyl and C(═O)NH2, and Ar is optionally substituted monocyclic or bicyclic aryl or heteroaryl, are useful as antitumor agents.;

主权项

1. A compound of formula wherein R1 is chosen from —(C3-C10)hydrocarbon, —O—(C3-C6)alkyl, and -A-R10, wherein A is a (C1-C6)hydrocarbon and R10 is chosen from —O—(C1-C6)alkyl, fluoro(C1-C6)alkyl, —O—(C1-C6)fluoroalkyl, hydroxy, —CN, nitro, —S—(C1-C6)alkyl, (C1-C6)alkoxycarbonyl, (C1-C6)acyl, amino, (C1-C6)alkylamino, di(C1-C6)alkylamino and (C1-C6)acylamino; and R2 is hydrogen; R3 is chosen from cyano, nitro, acetyl and —C(═O)NH2; R4 and R5 are independently chosen from hydrogen and methyl; Y is O; and Ar is chosen from;
a. phenyl substituted with from one to three substituents independently chosen from halogen, (C1-C10)hydrocarbon, fluoro(C1-C6)alkyl, —O(C1-C6)fluoroalkyl, —CN, nitro, (C1-C6)alkoxycarbonyl and (C1-C6)acyl; andb. naphthyl, and thiophenyl, either of which may be optionally substituted with from one to three substituents independently chosen from halogen, (C1-C10)hydrocarbon, fluoro(C1-C6)alkyl, —O(C1-C6)fluoroalkyl, —CN, nitro, (C1-C6)alkoxycarbonyl and (C1-C6)acyl.