SFX Get it!(opens in a new window)|View at Publisher| Export | Download | Add to List | More. BioMetals Volume 29, Issue 5, 1 October 2016, Pages 863-872 Organogold(III) compounds as experimental anticancer agents: chemical and biological profiles (Article) Massai, L.a , Cirri, D.a, Michelucci, E.b, Bartoli, G.c, Guerri, A.a, Cinellu, M.A.d, Cocco, F.d, Gabbiani, C.e, Messori, L.a a Department of Chemistry, University of Florence, Via Della Lastruccia 3, Sesto Fiorentino, Florence, Italy b Mass Spectrometry Center (CISM), University of Florence, Via U. Schiff 6, Sesto Fiorentino, Florence, Italy c Department of Experimental and Clinical Medicine, University of Florence, Viale GB Morgagni 50, Florence, Italy View additional affiliations View references (18) Abstract In the last few years gold(III) complexes have attracted growing attention in the medicinal chemistry community as candidate anticancer agents. In particular some organogold(III) compounds manifested quite attractive pharmacological behaviors in preclinical studies. Here we compare the chemical and biological properties of the novel organogold(III) complex [Au(bipydmb−H)(NH(CO)CH3)][PF6] (Aubipyaa) with those of its parent compounds [Au(bipydmb−H)(OH)][PF6] (Aubipyc) and [Au2(bipydmb−H)2)(μ−O)][PF6]2 (Au2bipyc), previously synthesized and characterized. The three study compounds were comparatively assessed for their antiproliferative actions against HCT-116 cancer cells, revealing moderate cytotoxic effects. Proapoptotic and cell cycle effects were also monitored. Afterward, to gain additional mechanistic insight, the three gold compounds were challenged against the model proteins HEWL, RNase A and cytochrome c and reactions investigated through UV–Vis and ESI–MS analysis. A peculiar and roughly invariant protein metalation profile emerges in the three cases consisting of protein binding of {Au(bipydmb−H)} moieties. The implications of these results are discussed in the frame of current knowledge on anticancer gold compounds.