ArticleJournal of medicinal chemistry2014
Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.
Article in Journal of medicinal chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed, 75 citations in OpenAlex.
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- Negative regulation of HDAC3 transcription by histone acetyltransferase TIP60 in colon cancer.Genes & genomics · 2024Article
- Discovery of novel and highly potent dual-targeting PKMYT1/HDAC2 inhibitors for hepatocellular carcinoma through structure-based virtual screening and biological evaluation.Frontiers in pharmacology · 2024Article
- Discovery of a Novel and Potent Dual-Targeting Inhibitor of ATM and HDAC2 Through Structure-Based Virtual Screening for the Treatment of Testicular Cancer.Drug design, development and therapy · 2024Article
- Discovery and biological evaluation of novel CARM1/HDAC2 dual-targeting inhibitors with anti-prostate cancer agents.Journal of enzyme inhibition and medicinal chemistry · 2023Article
- Targeting histone deacetylases for cancer therapy: Trends and challenges.Acta pharmaceutica Sinica. B · 2023Review
- Identification of novel and potent dual-targeting HDAC1/SPOP inhibitors using structure-based virtual screening, molecular dynamics simulation and evaluation ofFrontiers in pharmacology · 2023Article
- Concept of Hybrid Drugs and Recent Advancements in Anticancer Hybrids.Pharmaceuticals (Basel, Switzerland) · 2022Review
- Non-Hydroxamate Zinc-Binding Groups as Warheads for Histone Deacetylases.Molecules (Basel, Switzerland) · 2021Review
- Design, synthesis and evaluation of belinostat analogs as histone deacetylase inhibitors.Future medicinal chemistry · 2019Article
- Design, Synthesis and Biological Evaluation of Novel Osimertinib-Based HDAC and EGFR Dual Inhibitors.Molecules (Basel, Switzerland) · 2019Article
- Role of HDAC3-miRNA-CAGE Network in Anti-Cancer Drug-Resistance.International journal of molecular sciences · 2018Review
- The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity.European journal of medicinal chemistry · 2018Article
- Selective HDAC inhibitors with potent oral activity against leukemia and colorectal cancer: Design, structure-activity relationship and anti-tumor activity study.European journal of medicinal chemistry · 2017Article
- Design, synthesis and anti-tumor activity study of novel histone deacetylase inhibitors containing isatin-based caps and o-phenylenediamine-based zinc binding groups.Bioorganic & medicinal chemistry · 2017Article
- Regioselective Enzymatic Carboxylation of Bioactive (Poly)phenols.Advanced synthesis & catalysis · 2017Article
- Structural Requirements of HDAC Inhibitors: SAHA Analogues Modified at the C2 Position Display HDAC6/8 Selectivity.ACS medicinal chemistry letters · 2017Article
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Authors and funding
9 authors at 2 institutions in 2 countries.
Funding
Abstract
In our previous study, we designed and synthesized a novel series of N-hydroxycinnamamide-based HDAC inhibitors (HDACIs), among which the representative compound 14a exhibited promising HDACs inhibition and antitumor activity. In this current study, we report the development of a more potent class of N-hydroxycinnamamide-based HDACIs, using 14a as lead, among which, compound 11r gave IC50 values of 11.8, 498.1, 3.9, 2000.8, 5700.4, 308.2, and 900.4 nM for the inhibition of HDAC1, HDAC2, HDAC3, HDAC8, HDAC4, HDAC6, and HDAC11, exhibiting dual HDAC1/3 selectivity. Compounds 11e, 11r, 11w, and 11y showed excellent growth inhibition in multiple tumor cell lines. In vivo antitumor assay in U937 xenograft model identified compound 11r as a potent, orally active HDACI. To the best of our knowledge, this work constitutes the first report of oral active N-hydroxycinnamamide-based HDACIs with dual HDAC1/3 selectivity.
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Registered trials
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