N-heterocyclic carbene gold complexes with anticancer properties and methods of use thereof

摘要

Monomeric gold(I) complexes as anticancer agents. The gold(I) complexes are coordinated to mixed ligands: one N-heterocyclic carbene ligand and one monodentate dithiocarbamate-based ligand. Pharmaceutical compositions incorporating the gold(I) complexes, methods of synthesis, methods of treating cancer and methods of inhibiting cancer cell proliferation and inducing cancer cell apoptosis are also provided.

主权项

1. A N-heterocyclic carbene-gold(I) dithiocarbamate complex of formula I or a pharmaceutically acceptable salt, solvate, or prodrug thereof wherein: R1, R2, R3, R4, R5, R6, R7, R8 are each independently a hydrogen, an optionally substituted alkyl, an optionally substituted cycloalkyl, an optionally substituted heterocyclyl, an optionally substituted arylalkyl, an optionally substituted heteroaryl, an optionally substituted alkoxyl, an optionally substituted thioalkoxyl, an optionally substituted aryl, a N-monosubstituted amino group, or a N,N-disubstituted amino group; and R9 and R10 are each independently a hydrogen, an optionally substituted C1-C8 alkyl, an optionally substituted cycloalkyl, an optionally substituted heterocyclyl, an optionally substituted arylalkyl, an optionally substituted heteroaryl, an optionally substituted alkoxyl, an optionally substituted aryl, a N-monosubstituted amino group, or a N,N-disubstituted amino group; wherein the C1-C8 alkyl is optionally substituted with at least one substituent selected from the group consisting of hydroxyl, amino, alkylamino, arylamino, alkoxy, aryloxy, halo nitro, cyano, sulfonic acid, sulfate phosphonic acid, phosphate and phosphonate.