ArticleEuropean journal of medicinal chemistry2017
Selective HDAC inhibitors with potent oral activity against leukemia and colorectal cancer: Design, structure-activity relationship and anti-tumor activity study.
Article in European journal of medicinal chemistry, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed.
- Article
- Potential risks of histone deacetylase inhibitors in cancer therapeutics and feasible combination therapeutic strategies.World journal of clinical oncology · 2025Article
- Advancements in Hydrazide-Based HDAC Inhibitors: A Review of Recent Developments and Therapeutic Potential.Journal of medicinal chemistry · 2025Review
- Hitting Two Birds With One Stone: Dual Modulation of Brain Carbonic Anhydrases and Histone Deacetylases Boosts Memory Consolidation.Archiv der Pharmazie · 2025Article
- Can social adversity alter the epigenome, trigger oral disease, and affect future generations?Irish journal of medical science · 2024Review
- Targeting histone deacetylases for cancer therapy: Trends and challenges.Acta pharmaceutica Sinica. B · 2023Review
- Novel acetylation-related gene signatures for predicting the prognosis of patients with colorectal cancer.Human cell · 2022Article
- Development and Biological Evaluation of the First Highly Potent and Specific Benzamide-Based Radiotracer [Pharmaceuticals (Basel, Switzerland) · 2022Article
- Design and Synthesis of Hybrid Compounds as Epigenetic Modifiers.Pharmaceuticals (Basel, Switzerland) · 2021Article
- Non-Hydroxamate Zinc-Binding Groups as Warheads for Histone Deacetylases.Molecules (Basel, Switzerland) · 2021Review
- Role of HDAC6 and Its Selective Inhibitors in Gastrointestinal Cancer.Frontiers in cell and developmental biology · 2021Review
- Role of Histone Deacetylases in Monocyte Function in Health and Chronic Inflammatory Diseases.Reviews of physiology, biochemistry and pharmacology · 2021Review
- Class I HDAC Inhibitors Display Different Antitumor Mechanism in Leukemia and Prostatic Cancer Cells Depending on Their p53 Status.Journal of medicinal chemistry · 2018Article
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Authors and funding
13 authors.
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Abstract
Previously, we reported the discovery of a series of N-hydroxycinnamamide-based HDAC inhibitors, among which compound 11y exhibited high HDAC1/3 selectivity. In this current study, structural derivatization of 11y led to a new series of benzamide based HDAC inhibitors. Most of the compounds exhibited high HDACs inhibitory potency. Compound 11a (with 4-methoxybenzoyl as N-substituent in the cap and 4-(aminomethyl) benzoyl as the linker group) exhibited selectivity against HDAC1 to some extent, and showed potent antiproliferative activity against several tumor cell lines. In vivo studies revealed that compound 11a displayed potent oral antitumor activity in both hematological tumor cell U937 xenograft model and solid tumor cell HCT116 xenograft model with no obvious toxicity. Further modification of benzamide 3, 11a and 19 afforded new thienyl and phenyl compounds (50a, 50b, 63a, 63b and 63c) with dramatic HDAC1 and HDAC2 dual selectivity, and the fluorine containing compound 56, with moderate HDAC3 selectivity.
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