Spiroindoline-Capped Selective HDAC6 Inhibitors: Design, Synthesis, Structural Analysis, and Biological Evaluation

Author:

Saraswati A. Prasanth1,Relitti Nicola1ORCID,Brindisi Margherita1ORCID,Osko Jeremy D.2,Chemi Giulia1ORCID,Federico Stefano1,Grillo Alessandro1,Brogi Simone3ORCID,McCabe Niamh H.4,Turkington Richard C.4,Ibrahim Ola5,O’Sullivan Jeffrey5,Lamponi Stefania1,Ghanim Magda6,Kelly Vincent P.6,Zisterer Daniela6,Amet Rebecca6,Hannon Barroeta Patricia6,Vanni Francesca7,Ulivieri Cristina7,Herp Daniel8,Sarno Federica9,Di Costanzo Antonella9,Saccoccia Fulvio10,Ruberti Giovina10ORCID,Jung Manfred8ORCID,Altucci Lucia9,Gemma Sandra1ORCID,Butini Stefania1ORCID,Christianson David W.2ORCID,Campiani Giuseppe1ORCID

Affiliation:

1. Department of Biotechnology, Chemistry and Pharmacy, DoE Department of Excellence 2018-2022, University of Siena, via Aldo Moro 2, I-53100 Siena, Italy

2. Roy and Diana Vagelos Laboratories, Department of Chemistry, University of Pennsylvania, Philadelphia, Pennsylvania 19104-6323, United States

3. Department of Pharmacy, University of Pisa, via Bonanno 6, 56126, Pisa, Italy

4. Centre for Cancer Research and Cell Biology, Queens University Belfast, Belfast, U.K.

5. School of Dental Science, Trinity College Dublin, Lincoln Place, Dublin 2, Ireland

6. School of Biochemistry and Immunology, Trinity Biomedical Science Institute, Trinity College, 152-160, Pearse Street, Dublin 2, Ireland

7. Department of Life Sciences, University of Siena, via Aldo Moro 2, I-53100 Siena, Italy

8. Institute of Pharmaceutical Sciences, Albert-Ludwigs-Universität Freiburg, Albertstraße 25, 79104, Freiburg, Germany

9. Department of Precision Medicine, University of Campania “Luigi Vanvitelli″, 80138 Naples, Italy

10. Institute of Biochemistry and Cell Biology (IBBC), National Research Council (CNR), via E. Ramarini 32, 00015 Monterotondo, Rome, Italy

Funder

H2020 Marie Sklodowska-Curie Actions

European Cooperation in Science and Technology

Office of Science

Publisher

American Chemical Society (ACS)

Subject

Organic Chemistry,Drug Discovery,Biochemistry

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