Bioorganometallic fulvene-derived titanocene anti-cancer drugs

Strohfeldt, K. A. and Tacke, M. (2008) Bioorganometallic fulvene-derived titanocene anti-cancer drugs. Chemical Society Reviews, 37 (6). pp. 1174-1187. ISSN 0306-0012 doi: 10.1039/b707310k

Abstract/Summary

A review. 6-Substituted fulvenes are interesting and easily accessible starting materials for the synthesis of novel substituted titanocenes via reductive dimerization, carbolithiation or hydridolithiation reactions, which are followed by a transmetallation reaction with titanium tetrachloride in the latter two cases. Depending on the substitution pattern, these titanocenes prove to be bioorganometallic anticancer drugs, which have significant potential against advanced or metastatic renal-cell cancer. Patients bearing these stages of kidney cancer have a poor prognosis so far and therefore real progress in the area of metal-based anticancer drugs may come from this simple and effective synthetic approach. This tutorial review provides an insight into the synthesis of fulvene-derived titanocenes and their activity in preclin. expts.