Sixty years ago, the Australian chemist Francis P. Dwyer pioneered the use of ruthenium polypyridyl complexes as biologically active compounds. These chemically inert and configurationally stable complexes revealed an astonishing range of interesting biological activities, such as the inhibition of the enzyme acetylcholinesterase, anti-cancer activity in vivo, and bacteriostatic/bacteriocidal action. This review commemorates the sixtieth anniversary of Dwyer and co-workers’ landmark 1952 publication, summarises their broader achievements in biological inorganic chemistry, and discusses the contribution of this work to the development of modern biological and medicinal inorganic chemistry.