complex 8a

Complex 8a is an experimental organometallic gold(I) compound designed for targeted cancer therapy, specifically for ovarian cancer. It consists of a gold(I) N-heterocyclic carbene (NHC) core functionalized with a thiosugar moiety (1-thio-β-D-glucose tetraacetate) and bioconjugated to a [D-Lys6]-Luteinizing Hormone-Releasing Hormone (LHRH) targeting peptide. The thiosugar component is intended to enhance cellular uptake by exploiting the increased expression of glucose transporters (GLUTs) in cancer cells (the Warburg effect). The LHRH peptide moiety provides selectivity by targeting LHRH receptors, which are frequently overexpressed in ovarian and breast cancer cells. Mechanistically, the gold(I) center is believed to exert its cytotoxic effect primarily through the inhibition of thioredoxin reductase (TrxR), leading to oxidative stress and apoptosis. In preclinical studies, complex 8a has demonstrated potent cytotoxicity and improved selectivity in A2780 and SKOV-3 ovarian cancer cell lines compared to non-conjugated gold-NHC analogs.

Other names

LHRH-gold(I)-NHC-thiosugar conjugateAu(I)-NHC-thiosugar-LHRH conjugate