titanocene and Kidney-Neoplasms

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.

Topics: Animals; Antineoplastic Agents; Cell Survival; Cyclopentanes; Drug Screening Assays, Antitumor; Inhibitory Concentration 50; Kidney Neoplasms; LLC-PK1 Cells; Molecular Structure; Organometallic Compounds; Swine

Following promising recent in vitro and in vivo studies of the anticancer efficacies of heterometallic titanocene-gold chemotherapeutic candidates against renal cancer, we report here on the synthesis, characterization, stability studies and biological evaluation of a new titanocene complex containing a gold-triethylphosphane fragment [(η-C

Topics: Angiogenesis Inhibitors; Antineoplastic Agents; Cell Line, Tumor; Cell Movement; Cell Proliferation; Cell Survival; Coordination Complexes; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; Humans; Kidney Neoplasms; Molecular Conformation; Neovascularization, Pathologic; Organometallic Compounds; Phosphines; Structure-Activity Relationship

Titanocene difluorides can be obtained by halide metathesis of the respective titanocene dichlorides with trimethyltin fluoride (Me(3)SnF), giving access to a new class of cytotoxic active substances. Furthermore, an improved method for the synthesis of diaryl-substituted titanocene dichlorides is presented.

Topics: Animals; Antineoplastic Combined Chemotherapy Protocols; Apoptosis; Cell Line, Tumor; Cell Proliferation; Disease Models, Animal; Dose-Response Relationship, Drug; Drug Resistance, Neoplasm; Drug Screening Assays, Antitumor; Drug Synergism; Inhibitory Concentration 50; Kidney Neoplasms; LLC-PK1 Cells; Male; Mice; Mice, Nude; Molecular Structure; Neoplasm Transplantation; Organometallic Compounds; Prostatic Neoplasms; Proto-Oncogene Proteins c-bcl-2; Structure-Activity Relationship; Swine