2. Academic Validation
  3. 4,5,6,7-Tetrahydro-isoxazolo-[4,5-c]-pyridines as a new class of cytotoxic Hsp90 inhibitors

4,5,6,7-Tetrahydro-isoxazolo-[4,5-c]-pyridines as a new class of cytotoxic Hsp90 inhibitors

  • Eur J Med Chem. 2014 Apr 9:76:53-60. doi: 10.1016/j.ejmech.2014.01.056.
Riccardo Baruchello 1,  Daniele Simoni 2,  Paolo Marchetti 1,  Riccardo Rondanin 1,  Stefania Mangiola 1,  Cristiana Costantini 1,  Maria Meli 3,  Giuseppe Giannini 4,  Loredana Vesci 5,  Valeria Carollo 5,  Tiziana Brunetti 5,  Gianfranco Battistuzzi 5,  Manlio Tolomeo 6,  Walter Cabri 5
Affiliations

Affiliations

  • 1 Dipartimento di Scienze Chimiche e Farmaceutiche, Università degli Studi di Ferrara, I-44121 Ferrara, Italy.
  • 2 Dipartimento di Scienze Chimiche e Farmaceutiche, Università degli Studi di Ferrara, I-44121 Ferrara, Italy. Electronic address: smd@unife.it.
  • 3 Dipartimento di Scienze per la Promozione della Salute e Materno Infantile, Sezione di Farmacologia, Università di Palermo, Italy.
  • 4 R&D Sigma-Tau Industrie Farmaceutiche Riunite S.p.A., I-00040 Pomezia, Roma, Italy. Electronic address: giuseppe.giannini@sigma-tau.it.
  • 5 R&D Sigma-Tau Industrie Farmaceutiche Riunite S.p.A., I-00040 Pomezia, Roma, Italy.
  • 6 Centro Interdipartimentale di Ricerca in Oncologia Clinica e Dipartimento Biomedico di Medicina Interna e Specialistica, Sezione di Malattie Infettive, Università di Palermo, Palermo, Italy.
PMID: 24565573 DOI: 10.1016/j.ejmech.2014.01.056
Abstract

HSP90 is considered an interesting therapeutic target for Anticancer drug development. Here we describe a new class of 4,5,6,7-tetrahydro-isoxazolo-[4,5-c]-pyridine compounds. A small library of derivatives has been synthesized and investigated. Some reported compounds show interesting properties combining both notable binding to HSP90 and potent cell growth inhibitory activity. N-5 substitution with a 2,4 resorcinol carboxamide appears crucial for activity. Moreover, a derivative bearing a hydroxamic acid residue bound to C-3 amide portion was found to inhibit both HSP90 and HDAC6.

Keywords

4,5,6,7-Tetrahydro-isoxazolo-[4,5-c]-pyridines; Anti-cancer drugs; Heat shock protein 90.

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