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

Abstract : 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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Submitted on : Thursday, January 30, 2020 - 2:28:42 PM
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Martina de Pascale, Domenico Iacopetta, Marc Since, Sophie Corvaisier, V. Vié, et al.. Synthesis of Pyridoclax Analogues: Insight into Their Druggability by Investigating Their Physicochemical Properties and Interactions with Membranes. ChemMedChem, Wiley-VCH Verlag, 2020, 15 (1), pp.136-154. ⟨10.1002/cmdc.201900542⟩. ⟨hal-02434628⟩

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