Elisabetta Gabano, Mauro Ravera, Ilaria Zanellato, Stefano Tinello, Andrea Gallina, Beatrice Rangone, Valentina Gandin, Cristina Marzano, Maria Grazia Bottone, Domenico Osella
The design, synthesis, characterization and biological properties of a Pt(iv) complex containing the very active inhibitor of histone deacetylase (2-propynyl)octanoic acid, POA, as an axial ligand are reported here. The title complex, namely (OC-6-44)-acetatodiamminedichlorido(2-(2-propynyl)octanoato)platinum(iv), 1, containing POA in racemic or in enantiomeric forms, was one/two orders of magnitude more active than cisplatin, depending on the chemo-sensitivity of the cancer cell lines. Moreover, 1 exhibited similar or even better antiproliferative activity than (OC-6-33)-diamminedichloridobis(2-propylpentanoato)platinum(iv), 2, containing two molecules of the well-known histone deacetylase inhibitor 2-propylpentanoic (valproic) acid...
October 24, 2017: Dalton Transactions: An International Journal of Inorganic Chemistry