Identification of the key structural elements of a dihydropyrimidinone core driving toward more potent Hsp90 C-terminal inhibitors

S Terracciano; M G Chini; M C Vaccaro; M Strocchia; A Foglia; A Vassallo; C Saturnino; R Riccio; G Bifulco; I Bruno

doi:10.1039/c6cc06379a

Identification of the key structural elements of a dihydropyrimidinone core driving toward more potent Hsp90 C-terminal inhibitors

Chem Commun (Camb). 2016 Oct 25;52(87):12857-12860. doi: 10.1039/c6cc06379a.

Authors

S Terracciano, M G Chini¹, M C Vaccaro¹, M Strocchia¹, A Foglia¹, A Vassallo², C Saturnino¹, R Riccio¹, G Bifulco¹, I Bruno¹

Affiliations

¹ Department of Pharmacy, University of Salerno, via Giovanni Paolo II, 132, 84084, Fisciano, Italy. bifulco@unisa.it brunoin@unisa.it.
² Department of Science, University of Basilicata, Viale dell'Ateneo Lucano n.10, 85100 Potenza, Italy.

PMID: 27731433
DOI: 10.1039/c6cc06379a

Abstract

Hsp90 C-terminal modulation represents an attractive strategy for the development of potent and safer antitumor compounds. Continuing our investigation on DHPM type inhibitors here we report a new set of potent C-terminal ligands which allowed us to identify the key structural features crucial for the biological activity.