ANTI-CANCER COMPOUNDS

摘要

Quinazolines of the formula:- wherein R<1> is hydrogen or amino, or R<1> is alkyl, alkoxy or alkylthio each of up to 6 carbon atoms; or R<1> is aryl or aryloxy each of up to 10 carbon atoms; or R<1> is halogeno, hydroxy or mercapto; or R<1> 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 R<1> 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 R<2> is hydrogen or alkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, mercaptoalkyl, alkylthioalkyl, halogenoalkyl, cyanoalkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkyanoylalkyl, 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 carbomoyl and alkyl, alkoxy, halogenoalkyl, alkanoylamino, alkylthio and alkoxycarbonyl each of up to 6 carbon atoms; R<3> is the residue of a dipeptide in which the first, N-terminal amino acid residue thereof attached to the carbonyl group of COR<3> COR<3> is an L- or D-amino acid residue -NHCH(C2H)-A-CO- in which A is an alkylene group of up to 6 carbon atoms and the second amino acid residue is of an alpha -amino acid which has the D-configuration at its asymmetric alpha -carbon atom; wherein R<4> is hydrogen or alkyl of up to 4 carbon atoms; wherein R<5> is hydrogen or alkyl of up to 4 carbon atoms; and wherein each of R<6>, R<7> and R<8> is hydrogen or alkyl or alkoxy each of up to 4 carbon atoms; or is halogeno; or a pharmaceutically-acceptable salt, ester or amide thereof are of therapeutic value, particularly in the treatment of cancer.