Gold Complexes in Anticancer Therapy: From New Design Principles to Particle‐Based Delivery Systems

Abstract

The discovery of the medicinal properties of gold complexes has fuelled the design and synthesis of new anticancer metallodrugs, which have received special attention due to their unique modes of action. Current research in the development of gold compounds with therapeutic properties is predominantly focused on the molecular design of drug leads with superior pharmacological activities, e.g., by introducing targeting features. Moreover, intensive research aims at improving the physicochemical properties of gold compounds, such as chemical stability and solubility in the physiological environment. In this regard, the encapsulation of gold compounds in nanocarriers or their chemical grafting onto targeted delivery vectors could lead to new nanomedicines that eventually reach clinical applications. Herein, we provide an overview of the state‐of‐the‐art progress of gold anticancer compounds, andmore importantly we thoroughly revise the development of nanoparticle‐based delivery systems for gold chemotherapeutics.

Recent Advances in Metalloproteomics

“…Drugs such as aurothioglucose, aurothiomalate, and auranofin are based on Au(I) and, owing to their anti-inflammatory activity, are in current clinical use to combat arthritis. There is also vigorous research activity on Au(I)-and Au(III)-based anticancer agents [181][182][183]. Au(I) and Au(III) complexes are not kinetically inert and, indeed, their fast ligand exchange kinetics as well as their high likelihood to undergo reduction (especially in the reducing environment of the cytosols) has proven to be a bottleneck for bringing further gold-based drugs into the clinic.…”

Recent advances in anticancer drug discovery: A review

“…11 Aside from the complexity, first-hand treatments are extremely toxic and do not target cancer cells specifically. 12,13 This is true even though manufacturers are working on developing anticancer drugs. It is therefore of great interest to design and develop novel, selective small-molecule drugs, especially with the aid of in silico tools that have been developed in recent years.…”

Development of immunoliposomes containing cytotoxic gold payloads against HER2-positive breast cancers

“…14 In addition to classical chemotherapeutics (based on organic compounds and conventional platinum-based derivatives), gold compounds are emerging as potential anticancer agents due to their high cytotoxicity, unique mode of action, and immunogenic cell death generation. Nanoparticle-based delivery systems for gold chemotherapeutics have been recently reviewed, 15,16 but there are very few examples of goldcompound-based liposome systems. 17,18 We are interested in the development of targeted therapies for HER2-positive breast cancer.…”