In-Cell Activation of Organo-Osmium(II) Anticancer Complexes.

ABSTRACT: The family of iodido Os^II arene phenylazopyridine complexes [Os(η⁶ -p-cym)(5-R¹ -pyridylazo-4-R² -phenyl))I]⁺ (where p-cym=para-cymene) exhibit potent sub-micromolar antiproliferative activity towards human cancer cells and are active in vivo. Their chemical behavior is distinct from that of cisplatin: they do not readily hydrolyze, nor bind to DNA bases. We report here a mechanism by which they are activated in cancer cells, involving release of the I^- ligand in the presence of glutathione (GSH). The X-ray crystal structures of two active complexes are reported, 1-I (R¹ =OEt, R² =H) and 2-I (R¹ =H, R² =NMe₂ ). They were labelled with the radionuclide ¹³¹ I (β

SUBMITTER: Needham RJ 

PROVIDER: S-EPMC5412917 | biostudies-literature | 2017 Jan

REPOSITORIES: biostudies-literature