ArticleJournal of medicinal chemistry2013
Synthesis and structure-activity relationship of 3-hydroxypyridine-2-thione-based histone deacetylase inhibitors.
Article in Journal of medicinal chemistry, 2013. 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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Who cites it
14 citing papers in PubMed, 35 citations in OpenAlex.
- Crucial Structural Understanding for Selective HDAC8 Inhibition: Common Pharmacophores, Molecular Docking, Molecular Dynamics, and Zinc Binder Analysis of Selective HDAC8 Inhibitors.Medicinal chemistry (Shariqah (United Arab Emirates)) · 2025Review
- Hydroxypyrone derivatives in drug discovery: from chelation therapy to rational design of metalloenzyme inhibitors.RSC medicinal chemistry · 2022Review
- Review
- A versatile heterogeneous photocatalyst: nanoporous gold powder modified with a zinc(II) phthalocyanine derivative for singlet oxygen [4 + 2] cycloadditions.Photochemical & photobiological sciences : Official journal of the European Photochemistry Association and the European Society for Photobiology · 2021Article
- Comparison of the photocatalytic activity of novel hybrid photocatalysts based on phthalocyanines, subphthalocyanines and porphyrins immobilized onto nanoporous gold.RSC advances · 2021Article
- High Antiproliferative Activity of Hydroxythiopyridones over Hydroxypyridones and Their Organoruthenium Complexes.Biomedicines · 2021Article
- Impact of photosensitizer orientation on the distance dependent photocatalytic activity in zinc phthalocyanine-nanoporous gold hybrid systems.RSC advances · 2020Article
- Photocatalytic coatings based on a zinc(ii) phthalocyanine derivative immobilized on nanoporous gold leafs with various pore sizes.RSC advances · 2019Article
- Deferiprone: Pan-selective Histone Lysine Demethylase Inhibition Activity and Structure Activity Relationship Study.Scientific reports · 2019Article
- Targeting Metalloenzymes for Therapeutic Intervention.Chemical reviews · 2019Review
- Structural Requirements of HDAC Inhibitors: SAHA Analogues Modified at the C2 Position Display HDAC6/8 Selectivity.ACS medicinal chemistry letters · 2017Article
- Dual-Mode HDAC Prodrug for Covalent Modification and Subsequent Inhibitor Release.Journal of medicinal chemistry · 2015Article
- Histone deacetylase inhibitors in clinical studies as templates for new anticancer agents.Molecules (Basel, Switzerland) · 2015Review
- Design and structure activity relationship of tumor-homing histone deacetylase inhibitors conjugated to folic and pteroic acids.European journal of medicinal chemistry · 2015Article
Corrections and comments
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Authors and funding
5 authors at 2 institutions in 1 country.
Funding
Abstract
We previously identified 3-hydroxypyridine-2-thione (3HPT) as a novel zinc binding group for histone deacetylase (HDAC) inhibition. Early structure-activity relationship (SAR) studies led to various small molecules possessing selective inhibitory activity against HDAC6 or HDAC8 but devoid of HDAC1 inhibition. To delineate further the depth of the SAR of 3HPT-derived HDAC inhibitors (HDACi), we have extended the SAR studies to include the linker region and the surface recognition group to optimize the HDAC inhibition. The current efforts resulted in the identification of two lead compounds, 10d and 14e, with potent HDAC6 and HDAC8 activities that are inactive against HDAC1. These new HDACi possess anticancer activities against various cancer cell lines including Jurkat J.γ1 for which SAHA and the previously disclosed 3HPT-derived HDACi were inactive.
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Registered trials
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