Alkynyl phosphine gold complexes have potential as chemotherapeutics. A team of researchers from Germany and The Netherlands led by Ingo Ott, Technische Universität Braunschweig, Germany, prepared a series of six alkynyl gold(I) complexes and used them in biological assays. Proliferation assays showed the IC50 values of the complexes to be comparable with cytostatics such as cisplatin and 5-fluorouracil. According to an independent referee, these complexes comprise a promising new class of bioorganometallic anticancer drug candidates.
The compounds also act as thioredoxin reductase inhibitors, and have a significant effect on blood vessel formation in zebrafish embryos (pictured). Further investigations planned by the authors include the identification of further targets and the development of structure–activity relationships.
- On the Biological Properties of Alkynyl Phosphine Gold(I) Complexes,
Andreas Meyer, Christoph P. Bagowski, Malte Kokoschka, Maria Stefanopoulou, Hamed Alborzinia, Suzan Can, Danielle H. Vlecken, William S. Sheldrick, Stefan Wölfl, Ingo Ott,
Angew. Chem. Int. Ed. 2012, 51(35).
DOI: 10.1002/anie.201202939 - Angew. Chem. 2012, 124(35).
DOI: 10.1002/ange.201202939