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

S. Teracciano; 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†

S. Teracciano,^a M. G. Chini,^a M. C. Vaccaro,^a M. Strocchia,^a A. Foglia,^a A. Vassallo,^b C. Saturnino,^a R. Riccio,^a G. Bifulco ‡*^a and I. Bruno ‡*^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

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

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.

Chemical Communications

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

Abstract

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

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