Bioorganic & Medicinal Chemistry Letters 2009-05-15

Exploring bis-(indolyl)methane moiety as an alternative and innovative CAP group in the design of histone deacetylase (HDAC) inhibitors.

Giuseppe Giannini, Mauro Marzi, Maria Di Marzo, Gianfranco Battistuzzi, Riccardo Pezzi, Tiziana Brunetti, Walter Cabri, Loredana Vesci, Claudio Pisano

文献索引：Bioorg. Med. Chem. Lett. 19 , 2840, (2009)

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摘要

In order to gather further knowledge about the structural requirements on histone deacetylase inhibitors (HDACi), starting from the schematic model of the common pharmacophore that characterizes this class of molecules (surface recognition CAP group-connection unit-linker region-Zinc Binding Group), we designed and synthesized a series of hydroxamic acids containing a bis-(indolyl)methane moiety. HDAC inhibition profile and antiproliferative activity were evaluated.