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Chelate stabilization of a titanium(IV)–salan alkoxide by ligand exchange with 2,6-pyridinedicarboxylic acid (dipic) resulted in heptacoordinate complex 3 which is not redox-active, stable on silica gel and has increased aqueous stability. 3 is highly toxic in HeLa S3 and Hep G2 and has enhanced antitumor efficacy in a mouse cervical-cancer model.
Meitner-Auger-electron emitters have a promising potential for targeted radionuclide therapy of cancer because of their short range and the high linear energy transfer of Meitner-Auger-electrons (MAE). One promising MAE candidate is 197m/gHg with its half-life of 23.8 h and 64.1 h, respectively, and high MAE yield. Gold nanoparticles (AuNPs) that are labelled with 197m/gHg could be a helpful tool for radiation treatment of glioblastoma multiforme when infused into the surgical cavity after resection to prevent recurrence. To produce such AuNPs, 197m/gHg was embedded into pristine AuNPs. Two different syntheses were tested starting from irradiated gold containing trace amounts of 197m/gHg. When sodium citrate was used as reducing agent, no 197m/gHg labelled AuNPs were formed, but with tannic acid, 197m/gHg labeled AuNPs were produced. The method was optimized by neutralizing the pH (pH = 7) of the Au/197m/gHg solution, which led to labelled AuNPs with a size of 12.3 ± 2.0 nm as measured by transmission electron microscopy. The labelled AuNPs had a concentration of 50 μg (gold)/mL with an activity of 151 ± 93 kBq/mL (197gHg, time corrected to the end of bombardment).
Synthesis of derivatives of the peptide sequence L-pyroglutamyl-L-phenylalanyl-L-aspartyl-glycyl-L-lysyl-glycyl-glycyl-glycine as the antigenic determinant representing the N-terminal non-helical region of the α-2-chain of rabbit skin collagen, and conjugation to two different polypeptide carriers, are described.