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    Synthesis of Pyridoclax Analogues: Insight into Their Druggability by Investigating Their Physicochemical Properties and Interactions with Membranes

    Year: 2020

    Journal: ChemMedChem, Volume 15, JAN 7, page 136–154

    Authors: De Pascale, M; Iacopetta, D; Since, M; Corvaisier, S; Vie, V; Paboeuf, G; Hennequin, D; Perato, S; De Giorgi, M; Sinicropi, MS; Santos, JSD; Voisin-Chiret, AS; Malzert-Freon, A

    Organizations: Ligue Contre le Cancer (National committee); Ligue Contre le Cancer (Calvados committee); Commissione Europea; Fondo Sociale Europeo (FSE 2007/2013-PROGRAMMA ARUE); Regione CalabriaRegione Calabria; Region NormandieRegion Normandie; European Union via the European Regional Development Fund (FEDER)

    Keywords: Analytical methods; medicinal chemistry; membrane models; oligopyridines; structure-activity relationships

    Pyridoclax is considered a promising anticancer drug, acting as a protein-protein interaction disruptor, with potential applications in the treatment of ovarian, lung, and mesothelioma cancers. Eighteen sensibly selected structural analogues of Pyridoclax were synthesized, and their physicochemical properties were systematically assessed and analyzed. Moreover, considering that drug-membrane interactions play an essential role in understanding the mode of action of a given drug and its eventual toxic effects, membrane models were used to investigate such interactions in bulk (liposomes) and at the air-water interface. The measured experimental data on all original oligopyridines allowed the assessment of relative differences in terms of physicochemical properties, which could be determinant for their druggability, and hence for drug development.
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