Anticancer and antileishmanial in vitro activity of gold(I) complexes with 1,3,4‐oxadiazole‐2(3H)‐thione ligands derived from δ‐D‐gluconolactone

Abstract

Gold(I) complexes with saccharide-based ligands have been extensively studied in recent years, as they have shown significant in vitro cytotoxic activity against many cisplatin-resistant tumor cell lines (Rigobello et al., 2008). Unlike cisplatin, which targets DNA to exert its cytotoxic effect, gold(I) complexes interrupt intracellular protein signaling mechanisms (particularly thioredoxin reductase), leading to cell apoptosis (da Silva Maia, Deflon, & Abram, 2014). The structure of ligands used to synthesize gold(I) complexes has great influence on their biological activity (Yeo et al., 2013). An important factor is the lipophilicity of the ligand, which directly impacts the ability of the complex to penetrate through cell membranes. The insertion of a tertiary phosphine group in some gold(I) complexes (as in auranofin) has consistently resulted in increased biological activity, when compared to their analogous non-phosphorated compounds (Ott et al., 2009).

Novel Au Carbene Complexes as Promising Multi-Target Agents in Breast Cancer Treatment

“…In the last few years, several new gold complexes holding many biological activities have been reported [ 23 , 24 , 25 ], as well as the different intracellular targets, viz. kinases, proteases, reductases and, last but not least, topoisomerases [ 6 , 26 , 27 ].…”

The Ca2+-ATPase Inhibition Potential of Gold(I, III) Compounds

“…Thus, it was described that several inorganic compounds and complexes present Ca 2+ -ATPases IC 50 inhibition values globally not so different from the above well-known Ca 2+ -ATPases drugs inhibitors, for example decavanadate (IC 50 = 15 µM), polyoxotungstates (IC 50 = 0.3-200 µM), polyoxovanadates (IC 50 =1 µM), and vanadium complexes such as BMOV (IC 50 = 40 µM), among others [31][32][33][34][35]. In summary, both gold(I) and gold(III) compounds 1-4 are strong inhibitors of the SR Ca 2+ -ATPase, pointing out this enzyme as a putative target for gold compounds with anticancer activity, described as promising agents for the future in medicinal chemistry [1][2][3][4][5][6][7][8][9][10][11][12][13][14][15][16][17][18]23,29,[42][43][44].…”

Antimicrobial Activity of 1,3,4-Oxadiazole Derivatives

“…This form of the parasite is an important target in therapy. Additionally, the compounds displayed anticancer activity [94,95].…”

“…This form of the parasite is an important target in therapy. Additionally, the compounds displayed anticancer activity [94,95] 21), showed similar or better effect against Trypanosoma cruzi trypomastigotes in comparison to the standard drugs benznidazole and nifurtimox. Additionally, some compounds showed good antibacterial activity, while others showed antifungal activity [96].…”