Bioorganometallic fulvene-derived titanocene anti-cancer drugs.
6-Substituted fulvenes are interesting and easily accessible starting materials for the synthesis of novel substituted titanocenes via reductive dimerisation, 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 anti-cancer 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 anti-cancer 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 preclinical experiments.
Strohfeldt
Katja
K
School of Pharmacy, The University of Reading, PO Box 224, Whiteknights, Reading, Berkshire, UK. k.strohfeldt@reading.ac.uk
Tacke
Matthias
M
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002470:Cell Survival / Q000187:drug effects; D003517:Cyclopentanes / Q000737:chemistry*; D004354:Drug Screening Assays, Antitumor; D020128:Inhibitory Concentration 50; D007680:Kidney Neoplasms / Q000188:drug therapy*; D018374:LLC-PK1 Cells; D015394:Molecular Structure; D009942:Organometallic Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013552:Swine
D000970:Antineoplastic Agents; D003517:Cyclopentanes; D009942:Organometallic Compounds; C406884:titanocene; C017332:fulvene