146172-85-2

Upstream product

• 5893-05-0 Trt-Gly 
• 3197-06-6 N,N-bis(2-hydroxyethyl)ethylidenediamine 
• 146172-86-3 N-{[N',N'-bis-(2-hydroxyethyl)]-2-aminoethyl}-N''-tritylglycyl carboxamide 

Relevant academic research and scientific papers

Synthesis, structures and hypoxia-selective cytotoxicity of cobalt(III) complexes containing tridentate amine and nitrogen mustard ligands

Cobalt(in) complexes containing the tridentate nitrogen mustard ligand Ar, Ar-bis(2-chloroethyl)diethylenetriamine (DCD) and the non-alkylating analogs AW-diethyldiethylenetriamine (DED) and diethylenetriamine (dien) have been synthesised and the mustard complexes evaluated as potential hypoxia-selective anticancer drugs. The complexes were prepared from the precursor /ra/w-K.2[Co(acac)(CO3)(NO2)2]'H2O in a charcoal-catalyzed substitution reaction. Reaction of this precursor with dien-3HCl in water resulted in the isolation of two isomeric products, mer- and s-fac[Co(dien)(acac)(NO2)]f. Reaction in methanol with DED-3HC1 gave one product, ma complex containing DCD coordinated in a bidentate fashion, fra;w-Co(r|2-DCD)(acac)(NO2)2, were isolated. The two DCD complexes were characterized by X-ray structure determinations, which confirm the tridentate coordination with a long cobalt-tertiary nitrogen bond distance in the former, and bidentate coordination with the mustard nitrogen as a pendant arm in the latter. The bidentate complex, which contains a free nitrogen mustard, had cytotoxicity similar to that of the free ligand, but cytotoxicity was successfully masked in the tridentate complex, which showed modest hypoxic selectivity (five-fold) in a clonogenic assay. The Royal Society of Chemistry 2000.

Cobalt complexes as anti-cancer agents

New cobalt complexes of nitrogen mustard alkylating agents which have been found to have hypoxia-selective antitumour properties and are thereby useful antitumour agents are described.