Pt(iv) complexes based on cyclohexanediamines and the histone deacetylase inhibitor 2-(2-propynyl)octanoic acid: synthesis, characterization, cell penetration properties and antitumor activity

• DOI: 10.1039/d0dt04135a
• Publication Date: 2021-03-10T08:54:58Z
• Authors: Elisabetta Gabano; Beatrice Rangone; Elena Perin; Giulia Caron; Giuseppe Ermondi; Maura Vallaro; Valentina Gandin; Cristina Marzano; Alessandra Barban...; Nicola Margiotta; Mauro Ravera
• Keywords: Male; Organoplatinum Compounds; cisplatin; Drug Screening Assays; Inbred C57BL; Ligands; Antineoplastic Agent; Mice; Neoplasms; Histone Deacetylase Inhibitor; 0303 health sciences; Tumor; Molecular Structure; 3. Good health; kiteplatin; Female; Drug; Caprylates; Human; 610; Ligand; Antineoplastic Agents; histone deacetylase inhibitors; Diamines; Histone Deacetylases; Cell Line; Dose-Response Relationship; Experimental; Structure-Activity Relationship; 03 medical and health sciences; Cyclohexane; Histone Deacetylase; Cyclohexanes; Cell Line, Tumor; Animals; Humans; Cell Proliferation; Dose-Response Relationship, Drug; Animal; oxaliplatin; Organoplatinum Compound; Antitumor; Neoplasms, Experimental; 540; Histone Deacetylase Inhibitors; Mice, Inbred C57BL; Diamine; Caprylate; Drug Screening Assays, Antitumor; antitumor drugs; platinum complexes

Combinations of different cyclohexanediamines and 2-(2-propynyl)octanoate in Pt(iv) complexes resulted in prodrug candidates with promising antiproliferative and in vivo antitumor activity.