Targeting the Hsp90 C-terminal domain by the chemically accessible dihydropyrimidinone scaffold

Maria Strocchia; Stefania Terracciano; Maria G. Chini; Antonio Vassallo; Maria C. Vaccaro; Fabrizio Dal Piaz; Antonietta Leone; Raffaele Riccio; Ines Bruno; Giuseppe Bifulco

doi:10.1039/C4CC10074C

Targeting the Hsp90 C-terminal domain by the chemically accessible dihydropyrimidinone scaffold†

Maria Strocchia,‡^a Stefania Terracciano,‡^a Maria G. Chini,^a Antonio Vassallo,^b Maria C. Vaccaro,^a Fabrizio Dal Piaz,^a Antonietta Leone,^a Raffaele Riccio,^a Ines Bruno*^a and Giuseppe Bifulco*^a

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^a Department of Pharmacy, University of Salerno, via Giovanni Paolo II, 132, Fisciano, Italy
E-mail: bifulco@unisa.it, brunoin@unisa.it
Fax: +39 089 969602
Tel: +39 089 969741

^b Department of Science, University of Basilicata, Viale dell'Ateneo Lucano n.10, 85100 Potenza, Italy

Abstract

Hsp90 C-terminal ligands are potential new anti-cancer drugs alternative to the more studied N-terminal inhibitors. Here we report the identification of a new dihydropyrimidinone binding the C-terminus, which is not structurally related to other well-known natural and nature-inspired inhibitors of this second druggable Hsp90 site.

Chemical Communications

Targeting the Hsp90 C-terminal domain by the chemically accessible dihydropyrimidinone scaffold†

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Targeting the Hsp90 C-terminal domain by the chemically accessible dihydropyrimidinone scaffold

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