Discovery of salermide-related sirtuin inhibitors: binding mode studies and antiproliferative effects in cancer cells including cancer stem cells.

No abstract is available for this paper.

• Publication year

  2012

• Venue

  Journal of Medicinal Chemistry

• Publication date

  2012-12-12

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.1021/jm3011614PMID 23189967
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Pleiotropic effects of the sirtuin inhibitor sirtinol involves concentration‐dependent modulation of multiple nuclear receptor‐mediated pathways in androgen‐responsive prostate cancer cell LNCaP

  2013cited by this paper
• SIRT2 activity is required for the survival of C6 glioma cells.

  2012cited by this paper
• Cancer stem cells and novel targets for antitumor strategies.

  2012cited by this paper
• Cancer stem cells: an evolving concept

  2012cited by this paper
• Sirtuins and Disease: The Road Ahead

  2012cited by this paper
• Epigenetic protein families: a new frontier for drug discovery

  2012cited by this paper
• Sirtuin activators and inhibitors

  2012cited by this paper
• Mechanism-based modulator discovery for sirtuin-catalyzed deacetylation reaction.

  2012cited by this paper
• Sirtinol Treatment Reduces Inflammation in Human Dermal Microvascular Endothelial Cells

  2011cited by this paper
• Sirtuins: Molecular Traffic Lights in the Crossroad of Oxidative Stress, Chromatin Remodeling, and Transcription

  2011cited by this paper
• Sirtuin 1 (SIRT1)

  2011cited by this paper
• Acyl derivatives of p-aminosulfonamides and dapsone as new inhibitors of the arginine methyltransferase hPRMT1.

  2011cited by this paper
• SIRT1 modulation as a novel approach to the treatment of diseases of aging.

  2011cited by this paper
• HDAC6 and SIRT2 promote bladder cancer cell migration and invasion by targeting cortactin.

  2011cited by this paper
• Sirtuin 1 is upregulated in a subset of hepatocellular carcinomas where it is essential for telomere maintenance and tumor cell growth.

  2011cited by this paper
• SIRT2 down‐regulation in HeLa can induce p53 accumulation via p38 MAPK activation‐dependent p300 decrease, eventually leading to apoptosis

  2011cited by this paper
• Simplification of the tetracyclic SIRT1-selective inhibitor MC2141: coumarin- and pyrimidine-based SIRT1/2 inhibitors with different selectivity profile.

  2011cited by this paper
• Franklin H. Epstein Lecture: Sirtuins, aging, and medicine.

  2011cited by this paper
• Disruption of a Sirt1-dependent autophagy checkpoint in the prostate results in prostatic intraepithelial neoplasia lesion formation.

  2011cited by this paper
• Advances in characterization of human sirtuin isoforms: chemistries, targets and therapeutic applications.

  2011cited by this paper
• Enantioseparation of benzazoles and benzanilides on polysaccharide-based chiral columns.

  2010cited by this paper
• Mammalian sirtuins: biological insights and disease relevance.

  2010cited by this paper
• SIRT Inhibitors Induce Cell Death and p53 Acetylation through Targeting Both SIRT1 and SIRT2

  2010cited by this paper
• SIRT1: recent lessons from mouse models

  2010cited by this paper
• Inhibition of SIRT1 by a small molecule induces apoptosis in breast cancer cells.

  2010cited by this paper
• Identification of Tri‐ and Tetracyclic Pyrimidinediones as Sirtuin Inhibitors

  2010cited by this paper
• At the crossroad of lifespan, calorie restriction, chromatin and disease: Meeting on sirtuins

  2010cited by this paper
• Molecular Cancer Therapeutics SIRT Inhibitors Induce Cell Death and p 53 Acetylation through Targeting Both SIRT 1 and SIRT 2

  2010cited by this paper
• Sirtuins inhibitors: the approach to affinity and selectivity.

  2010cited by this paper
• Therapeutic potential of activators and inhibitors of sirtuins

  2010cited by this paper
• NAD+‐dependent histone deacetylases (sirtuins) as novel therapeutic targets

  2010cited by this paper
• Characterization of sirtuin inhibitors in nematodes expressing a muscular dystrophy protein reveals muscle cell and behavioral protection by specific sirtinol analogues.

  2010cited by this paper
• SIRT1 Histone Deacetylase Expression Is Associated with Microsatellite Instability and CpG Island Methylator Phenotype in Colorectal Cancer

  2009cited by this paper
• SirT1-null mice develop tumors at normal rates but are poorly protected by resveratrol

  2009cited by this paper
• Role of Sirtuin Histone Deacetylase SIRT1 in Prostate Cancer

  2009cited by this paper
• Salermide, a Sirtuin inhibitor with a strong cancer-specific proapoptotic effect

  2009cited by this paper
• Expression of DBC1 and SIRT1 Is Associated with Poor Prognosis of Gastric Carcinoma

  2009cited by this paper
• Expression and prognostic significance of SIRT1 in ovarian epithelial tumours

  2009cited by this paper
• Study of 1,4-dihydropyridine structural scaffold: discovery of novel sirtuin activators and inhibitors.

  2009cited by this paper
• SirT1 Is an Inhibitor of Proliferation and Tumor Formation in Colon Cancer*

  2009cited by this paper
• The SIRT1 Deacetylase Suppresses Intestinal Tumorigenesis and Colon Cancer Growth

  2008cited by this paper
• Mesenchymal differentiation of glioblastoma stem cells

  2008cited by this paper
• Impaired DNA damage response, genome instability, and tumorigenesis in SIRT1 mutant mice.

  2008cited by this paper
• Sirtuin 2 inhibitors rescue alpha-synuclein-mediated toxicity in models of Parkinson's disease.

  2007cited by this paper
• Sirtuin 2 Inhibitors Rescue α-Synuclein-Mediated Toxicity in Models of Parkinson's Disease

  2007cited by this paper
• Identification and expansion of human colon-cancer-initiating cells

  2007cited by this paper
• Discovery, In Vivo Activity, and Mechanism of Action of a Small-Molecule p53 Activator

  2007cited by this paper
• HATs and HDACs: from structure, function and regulation to novel strategies for therapy and prevention

  2007cited by this paper
• The epigenomics of cancer.

  2007cited by this paper
• Synthesis and biological evaluation of benzimidazole derivatives as potent AMP-activated protein kinase activators.

  2006cited by this paper
• Antitumor activity of a small-molecule inhibitor of human silent information regulator 2 enzymes.

  2006cited by this paper
• Inhibition of SIRT1 Catalytic Activity Increases p53 Acetylation but Does Not Alter Cell Survival following DNA Damage

  2006cited by this paper
• Histone deacetylation in epigenetics: An attractive target for anticancer therapy

  2005cited by this paper
• Design, synthesis, and biological evaluation of sirtinol analogues as class III histone/protein deacetylase (Sirtuin) inhibitors.

  2005cited by this paper
• Discovery of indoles as potent and selective inhibitors of the deacetylase SIRT1.

  2005cited by this paper
• Nutrient Availability Regulates SIRT1 Through a Forkhead-Dependent Pathway

  2004cited by this paper
• Absolute stereochemical determination of chiral carboxylic acids.

  2002cited by this paper
• Inhibition of Silencing and Accelerated Aging by Nicotinamide, a Putative Negative Regulator of Yeast Sir2 and Human SIRT1*

  2002cited by this paper
• Identification of a Class of Small Molecule Inhibitors of the Sirtuin Family of NAD-dependent Deacetylases by Phenotypic Screening*

  2001cited by this paper
• Translating the Histone Code

  2001cited by this paper

• Current Computational Approaches for the Discovery of Novel Anticancer Agents Targeting VEGFR and SIRT Signaling Pathways.

  2026cites this paper
• Sirtuin modulators: a review of patents from 2020 to 2024

  2025cites this paper
• Advancements in understanding the role and mechanism of sirtuin family (SIRT1-7) in breast cancer management.

  2025cites this paper
• Benzodeazaoxaflavin Sirtuin Inhibitors Inhibit Schistosoma mansoni Sirt2 and Cause Phenotypic Changes and Lethality in Schistosomula and Adult Worm Stages

  2025cites this paper
• Novel Anti-Cancer Stem Cell Compounds: A Comprehensive Review

  2024cites this paper
• SIRT1: a novel regulator in colorectal cancer.

  2024cites this paper
• Opportunities and Difficulties in the Repurposing of HDAC Inhibitors as Antiparasitic Agents

  2024cites this paper
• Uracil‐ and Pyridine‐Containing HDAC Inhibitors Displayed Cytotoxicity in Colorectal and Glioblastoma Cancer Stem Cells

  2024cites this paper
• Targeting sirtuins for cancer therapy: epigenetics modifications and beyond

  2024cites this paper
• Activation and inhibition of sirtuins: From bench to bedside

  2024cites this paper
• The influential responsibility of sirtuins in senescence and associated diseases: A review

  2024cites this paper
• Virtual Screening Combined with Enzymatic Assays to Guide the Discovery of Novel SIRT2 Inhibitors

  2023cites this paper
• Selective inhibition of SIRT2: A disputable therapeutic approach in cancer therapy.

  2023cites this paper
• Design and synthesis of sirtinol analogs as human neutrophil elastase inhibitors.

  2023cites this paper
• A pharmacological review on SIRT 1 and SIRT 2 proteins, activators, and inhibitors: Call for further research.

  2023cites this paper
• Virtual Screening in the Identification of Sirtuins’ Activity Modulators

  2022influential citation
• The sirtuin family in health and disease

  2022cites this paper
• Development of an Automated Screen for Kv7.2 Potassium Channels and Discovery of a New Agonist Chemotype.

  2022cites this paper
• Sirtuin modulators: past, present, and future perspectives.

  2022cites this paper
• Assessment of Pharmacological Interactions between SIRT2 Inhibitor AGK2 and Paclitaxel in Different Molecular Subtypes of Breast Cancer Cells

  2022cites this paper
• Sirtuins and the hallmarks of cancer

  2021cites this paper
• Discovery of 5-Benzylidene-2-phenyl-1,3-dioxane-4,6-diones as Highly Potent and Selective SIRT1 Inhibitors.

  2021cites this paper
• Emerging role of SIRT2 in non-small cell lung cancer

  2021influential citation
• Recent advances in the development of histone deacylase SIRT2 inhibitors

  2020cites this paper
• Novel SIRT Inhibitor, MHY2256, Induces Cell Cycle Arrest, Apoptosis, and Autophagic Cell Death in HCT116 Human Colorectal Cancer Cells

  2020cites this paper
• A novel chemical-combination screen in zebrafish identifies epigenetic small molecule candidates for the treatment of Duchenne muscular dystrophy

  2020cites this paper
• Biochemical mechanism and biological effects of the inhibition of silent information regulator 1 (SIRT1) by EX-527 (SEN0014196 or selisistat)

  2020cites this paper
• Exploring the newer oxadiazoles as real inhibitors of human SIRT2 in hepatocellular cancer cells.

  2020cites this paper
• Targeting histone acetylation/deacetylation in parasites: an update (2017-2020).

  2020cites this paper
• Emerging Role of Sirtuins in Breast Cancer Metastasis and Multidrug resistance: Implication for Novel Therapeutic Strategies Targeting Sirtuins.

  2020cites this paper
• Identification of Inhibitors to Trypanosoma cruzi Sirtuins Based on Compounds Developed to Human Enzymes

  2020cites this paper
• QSAR studies on the human sirtuin 2 inhibition by non-covalent 7,5,2-anilinobenzamide derivatives

  2020cites this paper
• The Versatility of Sirtuin-1 in Endocrinology and Immunology

  2020cites this paper
• Sirtuin modulators: where are we now? A review of patents from 2015 to 2019

  2020cites this paper
• Sirtuins as Drug Targets

  2019cites this paper
• Identification of novel quinazoline derivatives as potent antiplasmodial agents.

  2019cites this paper
• Dual Tumor Suppressor and Tumor Promoter Action of Sirtuins in Determining Malignant Phenotype

  2019cites this paper
• A Small‐Molecule SIRT2 Inhibitor That Promotes K‐Ras4a Lysine Fatty‐Acylation

  2019cites this paper
• Pharmacophore modeling and virtual screening studies to identify novel selective SIRT2 inhibitors.

  2019cites this paper
• Assessment of SIRT2 Inhibitors in Mouse Models of Cancer.

  2019cites this paper
• Development of Peptide-Based Sirtuin Defatty-Acylase Inhibitors Identified by the Fluorescence Probe, SFP3, That Can Efficiently Measure Defatty-Acylase Activity of Sirtuin.

  2019cites this paper
• Identification of Diketopiperazine-Containing 2-Anilinobenzamides as Potent Sirtuin 2 (SIRT2)-Selective Inhibitors Targeting the "Selectivity Pocket", Substrate-Binding Site, and NAD+-Binding Site.

  2019cites this paper
• SIRT2: Controversy and multiple roles in disease and physiology.

  2019cites this paper
• Structure-Reactivity Relationships on Substrates and Inhibitors of the Lysine Deacylase Sirtuin 2 from Schistosoma Mansoni (SmSirt2).

  2019cites this paper
• Sirtuins as novel targets in the pathogenesis of airway inflammation in bronchial asthma.

  2019cites this paper
• Enzymatic and Biological Characterization of Novel Sirtuin Modulators against Cancer

  2019cites this paper
• Colon cancer stemness as a reversible epigenetic state: Implications for anticancer therapies

  2019cites this paper
• PADI3 induces cell cycle arrest via the Sirt2/AKT/p21 pathway and acts as a tumor suppressor gene in colon cancer

  2019cites this paper
• Sirtuin Inhibitors and Activators

  2019cites this paper
• Role of Sirtuin1-p53 regulatory axis in aging, cancer and cellular reprogramming.

  2018cites this paper
• Breaking down the Contradictory Roles of Histone Deacetylase SIRT1 in Human Breast Cancer

  2018cites this paper
• Direct Comparison of SIRT2 Inhibitors: Potency, Specificity, Activity‐Dependent Inhibition, and On‐Target Anticancer Activities

  2018cites this paper
• Sirtuin 1 and oral cancer.

  2018cites this paper
• Lysine Deacetylase Inhibitors in Parasites: Past, Present, and Future Perspectives.

  2017cites this paper
• Sirtuins at the crossroads of stemness, aging, and cancer

  2017cites this paper
• Potent mechanism-based sirtuin-2-selective inhibition by an in situ-generated occupant of the substrate-binding site, “selectivity pocket” and NAD+-binding site

  2017cites this paper
• Highly Efficient Synthesis of Spirooxindole, Spiroacenaphthylene and Bisbenzo[b]pyran Derivatives and Evaluation of Their Inhibitory Activity against Sirtuin 2

  2017cites this paper
• Sirtuin Inhibition: Strategies, Inhibitors, and Therapeutic Potential.

  2017cites this paper
• Circadian Regulation of Colon Cancer Stem Cells: Implications for Therapy

  2016cites this paper
• Activity and mechanism of action of histone deacetylase inhibitors in synovial sarcoma

  2016cites this paper
• A SIRT2-Selective Inhibitor Promotes c-Myc Oncoprotein Degradation and Exhibits Broad Anticancer Activity.

  2016cites this paper
• 1,4-Dihydropyridines Active on the SIRT1/AMPK Pathway Ameliorate Skin Repair and Mitochondrial Function and Exhibit Inhibition of Proliferation in Cancer Cells.

  2016cites this paper
• A SIRT2-Selective Inhibitor Promotes c-Myc Oncoprotein Degradation and Exhibits Broad Anticancer Activity.

  2016cites this paper
• SIRT2 is an unfavorable prognostic biomarker in patients with acute myeloid leukemia

  2016cites this paper
• Sirtuin functions and modulation: from chemistry to the clinic

  2016cites this paper
• The SIRT2 Deacetylase Stabilizes Slug to Control Malignancy of Basal-like Breast Cancer.

  2016cites this paper
• Metal-binding effects of sirtuin inhibitor sirtinol

  2016cites this paper
• Histone acetyltransferase inhibitor CPTH6 preferentially targets lung cancer stem-like cells

  2016cites this paper
• Function of Sirtuins in Cancer Stem Cells

  2016cites this paper
• Histone deacetylase inhibitors for the treatment of cancer stem cells

  2016cites this paper
• Discovery of bicyclic pyrazoles as class III histone deacetylase SIRT1 and SIRT2 inhibitors.

  2015cites this paper
• Augmenting Antitumor Immune Responses with Epigenetic Modifying Agents

  2015cites this paper
• Sirtuin inhibitor sirtinol is an intracellular iron chelator.

  2015cites this paper
• Studying sirtuin inhibitors with in silico and in vitro approaches

  2015cites this paper
• New and under explored epigenetic modulators in search of new paradigms.

  2015cites this paper
• Design, synthesis and structure-activity relationship studies of novel sirtuin 2 (SIRT2) inhibitors with a benzamide skeleton.

  2015cites this paper
• Novel histone deacetylase inhibitors induce growth arrest, apoptosis, and differentiation in sarcoma cancer stem cells.

  2015cites this paper
• Functionalized tetrahydro-1H-pyrido[4,3-b]indoles: a novel chemotype with Sirtuin 2 inhibitory activity.

  2015cites this paper
• Virtual screening approach of sirtuin inhibitors results in two new scaffolds.

  2015cites this paper
• Characterization of Trypanosoma cruzi Sirtuins as Possible Drug Targets for Chagas Disease

  2015cites this paper
• Evaluation of benzoic acid derivatives as sirtuin inhibitors.

  2014cites this paper
• Discovery of potent and selective sirtuin 2 (SIRT2) inhibitors using a fragment-based approach.

  2014cites this paper
• Epigenetic drug discovery for Alzheimer’s disease

  2014cites this paper
• SIRT1 Inhibition Affects Angiogenic Properties of Human MSCs

  2014cites this paper
• Chemical metabolic inhibitors for the treatment of blood-borne cancers.

  2014cites this paper
• Getting to the Source: Selective Drug Targeting of Cancer Stem Cells

  2014cites this paper
• Sirtuin inhibitors as anticancer agents.

  2014cites this paper
• SIRT1 inhibition affects angiogenic properties of human MSCs.

  2014cites this paper
• Chroman-4-one- and chromone-based sirtuin 2 inhibitors with antiproliferative properties in cancer cells.

  2014cites this paper
• Development of Pyrazolone and Isoxazol-5-one Cambinol Analogues as Sirtuin Inhibitors

  2014cites this paper
• Development and characterization of 3-(benzylsulfonamido)benzamides as potent and selective SIRT2 inhibitors.

  2014cites this paper
• Structural insights of SIR2rp3 proteins as promising biotargets to fight against Chagas disease and leishmaniasis.

  2013cites this paper
• Screen of pseudopeptidic inhibitors of human sirtuins 1-3: two lead compounds with antiproliferative effects in cancer cells.

  2013cites this paper
• Sirtuin 1 and oral cancer ( Review )

  year unknowncites this paper