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Gold(I) complexes have emerged as versatile metallodrugs in medicinal inorganic chemistry with broad biological activity. Here we present selected results from collaborative studies on structurally diverse gold(I) compounds developed for anti-infective and anticancer applications. Phosphine-based complexes showed potent antiparasitic activity against Trypanosoma cruzi, reaching nanomolar IC₅₀ values and surpassing the reference drug by up to two orders of magnitude. Thiolate derivatives inspired by clinical gold drugs exhibited strong bactericidal effects against Gram-positive and Gram-negative strains. Azole-containing gold(I) complexes displayed antiproliferative activity against ovarian carcinoma cell lines, including drug-resistant phenotypes, as well as antifungal properties. Complementary spectroscopic and mass spectrometric studies were employed to investigate biomolecular interactions and provide insights into mechanisms of action, supporting their potential as multifunctional therapeutic leads in medicinal inorganic chemistry, highlighting their promise as multifunctional drug candidates.
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