Evaluation of azothioformamides and their copper(I) and silver(I) complexes for biological activity

Redox-active azothioformamides (ATFs) contain an NNCS 1,3-heterodiene motif typically found in other molecular subclasses that exhibit a wide range of cytotoxic and anti-neoplastic effects, either alone or as chelation complexes with various metals. For this study, a small library of ATF compounds was synthesized and tested across a range of microbes, fungi, and cancer cell lines for biological activity, both alone and as metal chelates of copper(I) and silver(I) salts. Alone, the ATF compounds exhibited little antimicrobial activity, but all inhibited the cell growth of A549 lung carcinoma cells (IC₅₀ values of 1-6 μM). As copper(I) and silver(I) coordination complexes, several of the ATFs showed antimicrobial activity against gram positive Staphylococcus aureus and Bacillus subtilis cells (IC₅₀ ∼ 5-20 μM) and the fungi Candida albicans (IC₅₀ ∼ 8-12 μM); as well as cytotoxicity against both lung carcinoma A549 cells and lymphoblastic leukemia K562 cells.