Structure–Activity Relationship of Propargylamine‐Based HDAC Inhibitors
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DOI: 10.1002/cmdc.201700550
Abstract: As histone deacetylases (HDACs) play an important role in the treatment of cancer, their selective inhibition has been the subject of various studies. These continuous investigations have given rise to a large collection of pan‐… read more here.
Keywords: relationship propargylamine; propargylamine based; hdac inhibitors; activity relationship ... See more keywords
Phenotypic Screening of Histone Deacetylase (HDAC) Inhibitors against Schistosoma mansoni
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DOI: 10.1002/cmdc.202100622
Abstract: Schistosomiasis is a prevalent yet neglected tropical parasitic disease caused by the Schistosoma genus of blood flukes. Praziquantel is the only currently available treatment, hence drug resistance poses a major threat. Recently, histone deacetylase 8… read more here.
Keywords: phenotypic screening; schistosoma mansoni; histone deacetylase; hdac inhibitors ... See more keywords
Nanosome-Mediated Delivery Of Hdac Inhibitors and Oxygen Molecules for the Transcriptional Reactivation of Latent Hiv-Infected Cd4+ T Cells.
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DOI: 10.1002/smll.202301730
Abstract: The treatment of human immunodeficiency virus (HIV) infection is notoriously difficult due to the ability of this virus to remain latent in the host's CD4+ T cells. Histone deacetylases (HDACs) interfere with DNA transcription in… read more here.
Keywords: cd4 cells; hdac inhibitors; hiv infected; drug ... See more keywords
Hydroxamic acid derivatives as histone deacetylase inhibitors: a DFT study of their tautomerism and metal affinities/selectivities
Sign Up to like & getrecommendations! Published in 2018 at "Journal of Molecular Modeling"
DOI: 10.1007/s00894-018-3651-6
Abstract: Hydroxamic acids are regarded as potent inhibitors of histone deacetylases (HDAC), and can therefore be used to reduce malignancy growth and size in affected organisms. Although there is a substantial body of information on the… read more here.
Keywords: hdac inhibitors; metal affinities; metal; affinities selectivities ... See more keywords
Targeting Histone Modifications in Bone and Lung Metastatic Cancers
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DOI: 10.1007/s11914-021-00670-2
Abstract: Breast cancer frequently metastasizes to the bone and lung, but the ability to treat metastatic tumor cells remains a pressing clinical challenge. Histone deacetylases (HDACs) and histone acetyltransferases (HATs) have emerged as promising targets since… read more here.
Keywords: bone lung; hdac inhibitors; metastatic cancers; lung metastatic ... See more keywords
HDAC Inhibitors Finally Open Up: Chromatin Accessibility Signatures of CTCL.
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DOI: 10.1016/j.ccell.2017.06.008
Abstract: In this issue of Cancer Cell, Qu et al. describe the chromatin accessibility profiles of cutaneous T cell lymphoma, with dynamic assessments of response and resistance to histone deacetylase inhibitor therapy. Their "personal regulome" analysis framework reveals… read more here.
Keywords: finally open; hdac inhibitors; accessibility; open chromatin ... See more keywords
HDAC inhibitors and cardioprotection: Homing in on a mechanism of action
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DOI: 10.1016/j.ebiom.2019.01.015
Abstract: Histone deacetylases (HDACs) are epigenetic regulators with imporConsistent with the observed reductions in apoptotic, oxidative stress tant roles in numerous cellular processes. The HDAC superfamily is divided into four classes based on function and sequence… read more here.
Keywords: vpa; cardiac remodelling; hdac inhibitors; infarct size ... See more keywords
Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies.
Sign Up to like & getrecommendations! Published in 2018 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2018.07.069
Abstract: This paper describes the rational development of a series of novel spiroindoline derivatives endowed with selective inhibitory activity on the HDAC6 isoform. A convenient multicomponent one-pot protocol was applied for the assembly of the desired… read more here.
Keywords: inhibitors synthesis; hdac inhibitors; novel spiroindoline; spiroindoline hdac ... See more keywords
Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2019.04.017
Abstract: A series of novel 2-aminobenzamide derivatives decorated with thioquinazolinone were designed and synthesized as histone deacetylase (HDAC) inhibitors. These derivatives were evaluated for their antiproliferative activities against several human cancer cell lines including A375, Hela,… read more here.
Keywords: novel; hdac inhibitors; deacetylase hdac; histone deacetylase ... See more keywords
Pragmatic recruitment of memantine as the capping group for the design of HDAC inhibitors: A preliminary attempt to unravel the enigma of glioblastoma.
Sign Up to like & getrecommendations! Published in 2021 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2021.113338
Abstract: Hurdled and marred by the notorious nature of glioblastomas (GBM) in terms of resistance to therapy and limited drug delivery into the brain, the anti-GBM drug pipeline is required to be loaded with mechanistically diverse… read more here.
Keywords: gbm; group; hdac inhibitors; gbm cells ... See more keywords
Epigenetic modulation and understanding of HDAC inhibitors in cancer therapy.
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DOI: 10.1016/j.lfs.2021.119504
Abstract: The role of genetic and epigenetic factors in tumor initiation and progression is well documented. Histone deacetylases (HDACs), histone methyl transferases (HMTs), and DNA methyl transferases. (DNMTs) are the main proteins that are involved in… read more here.
Keywords: understanding hdac; modulation understanding; hdac inhibitors; cancer ... See more keywords