Bioorganic Chemistry p. 43 - 56 (2018)
Update date:2022-08-15
Topics:
Shaaban, Saad
Vervandier-Fasseur, Dominique
Andreoletti, Pierre
Zarrouk, Amira
Richard, Philippe
Negm, Amr
Manolikakes, Georg
Jacob, Claus
Cherkaoui-Malki, Mustapha
Here a new series of twenty-one organoselenides, of potential protective activity, were synthesized and tested for their intrinsic cytotoxicity, anti-apoptotic and antioxidant capacities in oligodendrocytes. Most of the organoselenides were able to decrease the ROS levels, revealing antioxidant properties. Compounds 5b and 7b showed a high glutathione peroxidase (GPx)-like activities, which were 1.5 folds more active than ebselen. Remarkably, compound 5a diminished the formation of the oligodendrocytes SubG1 peak in a concentration-dependent manner, indicating its anti-apoptotic properties. Furthermore, based on the SwissADME web interface, we performed an in-silico structure-activity relationship to explore the drug-likeness of these organoselenides, predicting the pharmacokinetic parameters for compounds of interest that could cross the blood-brain barrier. Collectively, we present new organoselenide compounds with cytoprotective and antioxidant properties that can be considered as promising drug candidates for myelin diseases.
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Doi:10.1021/ja01206a506
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