DIPEPTIDYLQUINAZOLONES AS ANTI-CANCER AGENTS

摘要

Quinazolines of formula (I) wherein R1 is hydrogen or amino, or R1 is alkyl, alkoxy or alkylthio each of up to 6 carbon atoms; or R1 is aryl or aryloxy each of up to 10 carbon atoms; or R1 is halogeno, hydroxy or mercapto; or R1 is alkyl of up to 3 carbon atoms which bears one or more substituents selected from halogeno, hydroxy and alkanoylamino each of up to 6 carbon atoms; or R1 is alkoxy of up to 3 carbon atoms which bears one or more substituents selected from hydroxy and alkoxy of up to 6 carbon atoms; wherein R2 is hydrogen or alkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, mercaptoalkyl, alkylthioalkyl, halogenoalkyl, cyanoalkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkanoylalkyl, carboxyalkyl, carbamoylalkyl or alkanoyl each of up to 6 carbon atoms; wherein Ar is phenylene or heterocyclene which is unsubstituted or which bears one or more substituents selected from halogeno, cyano, nitro, hydroxy, amino and carbamoyl and alkyl, alkoxy, halogenoalkyl, alkanoylamino, alkylthio and alkoxycarbonyl each of up to 6 carbon atoms; R3 is the residue of a dipeptide in which the first, N-terminal amino acid residue thereof attached to the carbonyl group of COR3 is an amino acid residue (a) in which A is a carbon-carbon single bond or an alkylene group of up to 5 carbon atoms and V and V' are each separately hydrogen, or alkyl, alkenyl or alkynyl each of up to 6 carbon atoms; and the second amino acid residue is of an α-amino acid or a pharmaceutically-acceptable salt, ester or amide thereof are of therapeutic value, particularly in the treatment of cancer.