Squaramides as novel class I and IIB histone deacetylase inhibitors for topical treatment of cutaneous t-cell lymphoma.

Jean-François Fournier,Yushma Bhurruth-Alcor,Branislav Musicki,Jérome Aubert,Michèle Aurelly,Claire Bouix-Peter,Karinne Bouquet, Laurent Chantalat, Marion Delorme,Bénédicte Drean, Gwenaelle Duvert,Nicolas Fleury-Bregeot,Blanche Gauthier, Karine Grisendi,Craig S Harris,Laurent F Hennequin,Tatiana Isabet,Florence Joly,Guillaume Lafitte,Corinne Millois,Rémy Morgentin,Jonathan Pascau,David Piwnica,Yves Rival, Catherine Soulet, Étienne Thoreau,Loïc Tomas

Bioorganic & Medicinal Chemistry Letters（2018）

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摘要

•A novel squaramide-based scaffold for HDAC inhibition is proposed.•Inhibitors are optimized for topical route of administration.•Aqueous and organic solubility is optimized by crystal lattice perturbation.•Optimized HDAC inhibitors are class I, IIB and IV selective.

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XNBWKNWCSWBFRL-UHFFFAOYSA-N,WOGPSXAJPRAXBA-UHFFFAOYSA-N,RHUMXXCHLQENCI-UHFFFAOYSA-N

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