HIGHLY SELECTIVE INHIBITORS OF THE UROKINASE PLASMINOGEN ACTIVATOR

摘要

Aryl-guanidine derivatives (I), substituted by side-chains comprising hydrogen bond donor and acceptor groups, are new. Aryl-guanidines derivatives of formula (I) substituted by side-chains comprising hydrogen bond donor and acceptor groups, and their salts, are new. [Image] Ar : aromatic or heteroaromatic ring system; X1-CR3R4-C(=X2)-CR6R7R8, -NH-C(O)-CR6R7R8 or -CR3R4-C(=X2)-NHR8; R1H or (all optionally substituted) alkyl, alkenyl, alkynyl, aryl and/or heteroaryl; R2halo, -C(R3)3, -C(R3)2C(R3)3, -OC(R3)3 or -OC(R3)2C(R3)3; R3H or halo (especially F); R4 - R7H or (all optionally substituted) alkyl, alkenyl or alkynyl, R4 or R5 optionally being bonded with R6 or R7, provided that at least one of R4 and R5 and at least one of R6 and R7 contains a hydrogen bond donor group; R8H; alkyl, alkenyl, alkynyl, aryl and/or heteroaryl (all optionally substituted); or SO2R9; R9H or (all optionally substituted) alkyl, alkenyl, alkynyl, aryl and/or heteroaryl; X2hydrogen bond acceptor group, especially NH, NR10, O or S; R10alkyl, alkenyl or alkynyl (all optionally substituted); and m : 0-4. - ACTIVITY : Cytostatic. No biological data given. - MECHANISM OF ACTION : Urokinase plasminogen activator (uPA) inhibitor; urokinase (UK) inhibitor