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Bioorg Med Chem Lett. 2018 Sep 15;28(17):2985-2992. doi: 10.1016/j.bmcl.2018.06.029. Epub 2018 Jun 18.

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

Author information

1
Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France. Electronic address: jean-francois.fournier@umontreal.ca.
2
Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France.
3
Edelris, 115 Avenue Lacassagne, 69003 Lyon, France.
4
Synchrotron Soleil, L'Orme des Merisiers, Saint-Aubin - BP 48, 91192 Gif-sur-Yvette Cedex, France.

Abstract

A series of squaramide-based hydroxamic acids were designed, synthesized and evaluated against human HDAC enzyme. Squaramides were found to be potent in the Hut78 cell line, but initially suffered from low solubility. Leads with improved solubility and metabolic profiles were shown to be class I, IIB and IV selective.

KEYWORDS:

CTCL; HDAC inhibitors; Mycosis fungoides; Squaramide; Topical

PMID:
30122227
DOI:
10.1016/j.bmcl.2018.06.029
[Indexed for MEDLINE]

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