ArticleJournal of medicinal chemistry2012
Synthesis and biological evaluation of 1-arylsulfonyl-5-(N-hydroxyacrylamide)indoles as potent histone deacetylase inhibitors with antitumor activity in vivo.
Article in Journal of medicinal chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
18 citing papers in PubMed.
- Role of Histone Deacetylase and Inhibitors in Cardiovascular Diseases.Cell proliferation · 2025Review
- The epigenetic landscape of rheumatoid arthritis: Pathogenesis and drug therapeutic potentials.Acta pharmaceutica Sinica. B · 2025Review
- Iodine-mediated synthesis of indolyl-1,3,4-thiadiazole amine derivatives and their DFT analysis.RSC advances · 2025Article
- Modulation of Abnormal Vasoconstriction Through 2-Hydroxyisobutyrylation of Tropomyosin 3 Lys141: Targeting Histone Deacetylase 3 as a Key Approach.Journal of the American Heart Association · 2025Article
- Targeting histone deacetylase in cardiac diseases.Frontiers in physiology · 2024Review
- Epigenetic reactivation of tumor suppressor genes with CRISPRa technologies as precision therapy for hepatocellular carcinoma.Clinical epigenetics · 2023Article
- Design, synthesis, and structure activity relationship analysis of new betulinic acid derivatives as potent HIV inhibitors.European journal of medicinal chemistry · 2021Article
- Role of Indole Scaffolds as Pharmacophores in the Development of Anti-Lung Cancer Agents.Molecules (Basel, Switzerland) · 2020Review
- Combination treatment strategy for pancreatic cancer involving the novel HDAC inhibitor MPT0E028 with a MEK inhibitor beyond K-Ras status.Clinical epigenetics · 2019Article
- TIMP3 expression associates with prognosis in colorectal cancer and its novel arylsulfonamide inducer, MPT0B390, inhibits tumor growth, metastasis and angiogenesis.Theranostics · 2019Article
- Methods for Hydroxamic Acid Synthesis.Current organic chemistry · 2019Article
- Human histone deacetylase 6 shows strong preference for tubulin dimers over assembled microtubules.Scientific reports · 2017Article
- Structure based design, synthesis and activity studies of small hybrid molecules as HDAC and G9a dual inhibitors.Oncotarget · 2017Article
- Article
- Structural Optimization of Indole Derivatives Acting at Colchicine Binding Site as Potential Anticancer Agents.ACS medicinal chemistry letters · 2015Article
- Exploration of Novel Inhibitors for Class I Histone Deacetylase Isoforms by QSAR Modeling and Molecular Dynamics Simulation Assays.PloS one · 2015Article
- A novel action mechanism for MPT0G013, a derivative of arylsulfonamide, inhibits tumor angiogenesis through up-regulation of TIMP3 expression.Oncotarget · 2014Article
- Development ofACS medicinal chemistry letters · 2013Article
Corrections and comments
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Authors and funding
12 authors.
Funding
Abstract
A series of 1-arylsulfonyl-5-(N-hydroxyacrylamide)indoles has been identified as a new class of histone deacetylase inhibitors. Compounds 8, 11, 12, 13, and 14 demonstrated stronger antiproliferative activities than 1 (SAHA) with GI(50) values ranging from 0.36 to 1.21 μM against Hep3B, MDA-MB-231, PC-3, and A549 human cancer cell lines. Lead compound 8 showed remarkable HDAC 1, 2, and 6 isoenzymes inhibitory activities with IC(50) values of 12.3, 4.0, 1.0 nM, respectively, which are comparable to 1. In in vivo efficacy evaluation against lung A549 xenograft model, 8 displayed better antitumor activity than compound 1.
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Registered trials
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.