ArticleACS medicinal chemistry letters2020
Spiroindoline-Capped Selective HDAC6 Inhibitors: Design, Synthesis, Structural Analysis, and Biological Evaluation.
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Article in ACS medicinal chemistry letters, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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14citing papers in PubMed
2.0field-weighted citation impact, top 13% of its field
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Who cites it
14 citing papers in PubMed, 39 citations in OpenAlex.
- Recent Advances in the Synthesis of Spiroindolines: Catalytic Strategies, Stereoselectivity, and Synthetic Utility (2020-2025).Molecules (Basel, Switzerland) · 2026Review
- Taginostat, a new quinolone-based HDAC6 inhibitor, promotes apoptosis of chronic lymphocytic leukemia cells in vitro and in vivo by activating STAT4.Apoptosis : an international journal on programmed cell death · 2026Article
- Discovery of thieno[2,3-RSC advances · 2026Article
- Synthesis and crystal structure of HDAC6 selective inhibitor ofActa crystallographica. Section E, Crystallographic communications · 2026Article
- Spirotetrahydroisoquinoline-Based Histone Deacetylase Inhibitors as New Antifibrotic Agents: Biological Evaluation in Human Fibroblasts from Bronchoalveolar Lavages of Idiopathic Pulmonary Fibrosis Patients.ACS pharmacology & translational science · 2025Article
- Design, synthesis, biological andBiomedical reports · 2025Article
- Repurposing of known drugs from multiple libraries to identify novel and potential selective inhibitors of HDAC6 viaHeliyon · 2024Article
- Development of Epigenetic Modifiers with Therapeutic Potential in FMS-Related Tyrosine Kinase 3/Internal Tandem Duplication (FLT3/ITD) Acute Myeloid Leukemia and Other Blood Malignancies.ACS pharmacology & translational science · 2024Article
- Effects of structurally distinct human HDAC6 and HDAC6/HDAC8 inhibitors against S. mansoni larval and adult worm stages.PLoS neglected tropical diseases · 2024Article
- Rational design of synthetically tractable HDAC6/HSP90 dual inhibitors to destroy immune-suppressive tumor microenvironment.Journal of advanced research · 2023Article
- Diastereoselective Synthesis ofACS omega · 2022Article
- A Therapeutic Perspective of HDAC8 in Different Diseases: An Overview of Selective Inhibitors.International journal of molecular sciences · 2022Review
- Chasing a Breath of Fresh Air in Cystic Fibrosis (CF): Therapeutic Potential of Selective HDAC6 Inhibitors to Tackle Multiple Pathways in CF Pathophysiology.Journal of medicinal chemistry · 2022Review
- Harnessing the Role of HDAC6 in Idiopathic Pulmonary Fibrosis: Design, Synthesis, Structural Analysis, and Biological Evaluation of Potent Inhibitors.Journal of medicinal chemistry · 2021Article
Corrections and comments
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Authors and funding
31 authors at 8 institutions in 5 countries.
A Prasanth SaraswatiDepartment of Biotechnology, Chemistry and Pharmacy, DoE Department of Excellence 2018-2022, University of Siena, via Aldo Moro 2, I-53100 Siena, Italy.
Nicola RelittiDepartment of Biotechnology, Chemistry and Pharmacy, DoE Department of Excellence 2018-2022, University of Siena, via Aldo Moro 2, I-53100 Siena, Italy.
Margherita BrindisiDepartment of Biotechnology, Chemistry and Pharmacy, DoE Department of Excellence 2018-2022, University of Siena, via Aldo Moro 2, I-53100 Siena, Italy.
Jeremy D OskoRoy and Diana Vagelos Laboratories, Department of Chemistry, University of Pennsylvania, Philadelphia, Pennsylvania 19104-6323, United States.
Giulia ChemiDepartment of Biotechnology, Chemistry and Pharmacy, DoE Department of Excellence 2018-2022, University of Siena, via Aldo Moro 2, I-53100 Siena, Italy.
Stefano FedericoDepartment of Biotechnology, Chemistry and Pharmacy, DoE Department of Excellence 2018-2022, University of Siena, via Aldo Moro 2, I-53100 Siena, Italy.
Alessandro GrilloDepartment of Biotechnology, Chemistry and Pharmacy, DoE Department of Excellence 2018-2022, University of Siena, via Aldo Moro 2, I-53100 Siena, Italy.
Simone BrogiDepartment of Pharmacy, University of Pisa, via Bonanno 6, 56126, Pisa, Italy.
Niamh H McCabeCentre for Cancer Research and Cell Biology, Queens University Belfast, Belfast, U.K.
Richard C TurkingtonCentre for Cancer Research and Cell Biology, Queens University Belfast, Belfast, U.K.
Ola IbrahimSchool of Dental Science, Trinity College Dublin, Lincoln Place, Dublin 2, Ireland.
Jeffrey O'SullivanSchool of Dental Science, Trinity College Dublin, Lincoln Place, Dublin 2, Ireland.
Stefania LamponiDepartment of Biotechnology, Chemistry and Pharmacy, DoE Department of Excellence 2018-2022, University of Siena, via Aldo Moro 2, I-53100 Siena, Italy.
Magda GhanimSchool of Biochemistry and Immunology, Trinity Biomedical Science Institute, Trinity College, 152-160, Pearse Street, Dublin 2, Ireland.
Vincent P KellySchool of Biochemistry and Immunology, Trinity Biomedical Science Institute, Trinity College, 152-160, Pearse Street, Dublin 2, Ireland.
Daniela ZistererSchool of Biochemistry and Immunology, Trinity Biomedical Science Institute, Trinity College, 152-160, Pearse Street, Dublin 2, Ireland.
Rebecca AmetSchool of Biochemistry and Immunology, Trinity Biomedical Science Institute, Trinity College, 152-160, Pearse Street, Dublin 2, Ireland.
Patricia Hannon BarroetaSchool of Biochemistry and Immunology, Trinity Biomedical Science Institute, Trinity College, 152-160, Pearse Street, Dublin 2, Ireland.
Francesca VanniDepartment of Life Sciences, University of Siena, via Aldo Moro 2, I-53100 Siena, Italy.
Cristina UlivieriDepartment of Life Sciences, University of Siena, via Aldo Moro 2, I-53100 Siena, Italy.
Daniel HerpInstitute of Pharmaceutical Sciences, Albert-Ludwigs-Universität Freiburg, Albertstraße 25, 79104, Freiburg, Germany.
Federica SarnoDepartment of Precision Medicine, University of Campania "Luigi Vanvitelli″, 80138 Naples, Italy.
Antonella Di CostanzoDepartment of Precision Medicine, University of Campania "Luigi Vanvitelli″, 80138 Naples, Italy.
Fulvio SaccocciaInstitute of Biochemistry and Cell Biology (IBBC), National Research Council (CNR), via E. Ramarini 32, 00015 Monterotondo, Rome, Italy.
Giovina RubertiInstitute of Biochemistry and Cell Biology (IBBC), National Research Council (CNR), via E. Ramarini 32, 00015 Monterotondo, Rome, Italy.
Manfred JungInstitute of Pharmaceutical Sciences, Albert-Ludwigs-Universität Freiburg, Albertstraße 25, 79104, Freiburg, Germany.
Lucia AltucciDepartment of Precision Medicine, University of Campania "Luigi Vanvitelli″, 80138 Naples, Italy.
Sandra GemmaDepartment of Biotechnology, Chemistry and Pharmacy, DoE Department of Excellence 2018-2022, University of Siena, via Aldo Moro 2, I-53100 Siena, Italy.
Stefania ButiniDepartment of Biotechnology, Chemistry and Pharmacy, DoE Department of Excellence 2018-2022, University of Siena, via Aldo Moro 2, I-53100 Siena, Italy.
David W ChristiansonRoy and Diana Vagelos Laboratories, Department of Chemistry, University of Pennsylvania, Philadelphia, Pennsylvania 19104-6323, United States.
Giuseppe CampianiDepartment of Biotechnology, Chemistry and Pharmacy, DoE Department of Excellence 2018-2022, University of Siena, via Aldo Moro 2, I-53100 Siena, Italy.
University of Siena · ITTrinity College Dublin · IEUniversity of Campania "Luigi Vanvitelli" · ITNational Research Council · ITQueens University · BDUniversity of Freiburg · DEUniversity of Pennsylvania · USUniversity of Pisa · IT
Funding
User Training and OutreachP30GM124165 · NIGMS · CORNELL UNIVERSITY · PI MALCOLM S. CAPEL · 2018 to 2026
$34.2MStructure and Function of MetalloenzymesR01GM049758 · NIGMS · UNIVERSITY OF PENNSYLVANIA · PI CHRISTIANSON, DAVID W · 1994 to 2025
$7.6MPixel Array Detector for X-ray CrystallographyS10RR029205 · NCRR · CORNELL UNIVERSITY · PI EALICK, STEVEN E · 2010 to 2010
$1.8MNCRR NIH HHS S10 RR029205NIGMS NIH HHS P30 GM124165NIGMS NIH HHS R01 GM049758
Abstract
Histone deacetylase inhibitors (HDACi) have emerged as promising therapeutics for the treatment of neurodegeneration, cancer, and rare disorders. Herein, we report the development of a series of spiroindoline-based HDAC6 isoform-selective inhibitors based on the X-ray crystal studies of the hit
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.