Medicinal chemistry updates of novel HDACs inhibitors (2020 to present)

Studying Histone Deacetylase Inhibition and Apoptosis Induction of Psammaplin A Monomers with Modified Thiol Group

(2021) Yu Bao et al.   ACS Medicinal Chemistry Letters

Design, synthesis and antitumor activity evaluation of novel HDAC inhibitors with tetrahydrobenzothiazole as the skeleton

(2021) Simin Sun et al.   BIOORGANIC CHEMISTRY

Pragmatic recruitment of Memantine as the capping group for the Design of HDAC inhibitors: A preliminary attempt to unravel the enigma of Glioblastoma

(2021) Kunal Nepali et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

An update on the emerging approaches for histone deacetylase (HDAC) inhibitor drug discovery and future perspectives

(2021) Ma Su et al.   Expert Opinion on Drug Discovery

Unique Molecular Interaction with the Histone Deacetylase 6 Catalytic Tunnel: Crystallographic and Biological Characterization of a Model Chemotype

(2021) Olasunkanmi O. Olaoye et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Novel Plasmodium falciparum HDAC1 Inhibitors with Dual-Stage Antimalarial Potency and Improved Safety Based on the Clinical Anticancer Drug Candidate Quisinostat

(2021) Ruoxi Li et al.   JOURNAL OF MEDICINAL CHEMISTRY

HDAC7 Inhibition by Phenacetyl and Phenylbenzoyl Hydroxamates

(2021) Jeffrey Y. W. Mak et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis of HDAC Inhibitor Libraries via Microscale Workflow

(2021) Kevin D. Dykstra et al.   ACS Medicinal Chemistry Letters

Evaluation of 5-(Trifluoromethyl)-1,2,4-oxadiazole-Based Class IIa HDAC Inhibitors for Huntington’s Disease

(2021) Andrew J. Stott et al.   ACS Medicinal Chemistry Letters

Redefining the Histone Deacetylase Inhibitor Pharmacophore: High Potency with No Zinc Cofactor Interaction

(2021) Douglas C. Beshore et al.   ACS Medicinal Chemistry Letters

Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors

(2021) Maurício Temotheo Tavares et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Discovery of Ethyl Ketone-Based Highly Selective HDACs 1, 2, 3 Inhibitors for HIV Latency Reactivation with Minimum Cellular Potency Serum Shift and Reduced hERG Activity

(2021) Wensheng Yu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Tetrahydroquinoline-Capped Histone Deacetylase 6 Inhibitor SW-101 Ameliorates Pathological Phenotypes in a Charcot–Marie–Tooth Type 2A Mouse Model

(2021) Sida Shen et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of macrocyclic HDACs 1, 2, and 3 selective inhibitors for HIV latency reactivation

(2021) Wensheng Yu et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis, biological evaluation, and molecular docking analysis of novel linker-less benzamide based potent and selective HDAC3 inhibitors

(2021) Ganesh Routholla et al.   BIOORGANIC CHEMISTRY

Identification of novel 1,3-diaryl-1,2,4-triazole-capped histone deacetylase 6 inhibitors with potential anti-gastric cancer activity

(2021) Xin-Hui Zhang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and biological evaluation of phenothiazine derivative-containing hydroxamic acids as potent class II histone deacetylase inhibitors

(2021) Kai-Cheng Hsu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design, synthesis and biological evaluation of brain penetrant benzazepine-based histone deacetylase 6 inhibitors for alleviating stroke-induced brain infarction

(2021) Zheng Guo et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Development of HDAC Inhibitors Exhibiting Therapeutic Potential in T-Cell Prolymphocytic Leukemia

(2021) Krimo Toutah et al.   JOURNAL OF MEDICINAL CHEMISTRY

Pyrimethamine conjugated histone deacetylase inhibitors: Design, synthesis and evidence for triple negative breast cancer selective cytotoxicity

(2020) Bocheng Wu et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Synthesis and biological evaluation of 6-phenylpurine linked hydroxamates as novel histone deacetylase inhibitors

(2020) Dizhong Chen et al.   BIOORGANIC CHEMISTRY

Histone deacetylase (HDAC) inhibitors in cancer: a patent review (2017-present)

(2020) Chunlong Zhao et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Novel Selective Histone Deacetylase 6 (HDAC6) Inhibitors: A Patent Review (2016-2019)

(2020) Xingrui He et al.   Recent Patents on Anti-Cancer Drug Discovery

Synthesis and biological evaluation of acridine-based histone deacetylase inhibitors as multitarget agents against Alzheimer’s disease

(2020) Hui-Ju Tseng et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening

(2020) Jian Liu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Achiral Derivatives of Hydroxamate AR-42 Potently Inhibit Class I HDAC Enzymes and Cancer Cell Proliferation

(2020) Jiahui Tng et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity

(2020) Xiaoyang Li et al.   JOURNAL OF MEDICINAL CHEMISTRY

Development of Selective Histone Deacetylase 6 (HDAC6) Degraders Recruiting Von Hippel–Lindau (VHL) E3 Ubiquitin Ligase

(2020) Ka Yang et al.   ACS Medicinal Chemistry Letters

Hydroxamic Acids Immobilized on Resins (HAIRs): A Toolbox for the Synthesis of Dual‐Targeting HDAC Inhibitors and HDAC Degraders (PROTACs)

(2020) Laura Sinatra et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Exploration of certain 1,3-oxazole- and 1,3-thiazole-based hydroxamic acids as histone deacetylase inhibitors and antitumor agents

(2020) Duong Tien Anh et al.   BIOORGANIC CHEMISTRY

Design, synthesis and biological evaluation of coumarin-based N-hydroxycinnamamide derivatives as novel histone deacetylase inhibitors with anticancer activities

(2020) Jiaoli Ding et al.   BIOORGANIC CHEMISTRY

Purine/purine isoster based scaffolds as new derivatives of benzamide class of HDAC inhibitors

(2020) Kunal Nepali et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design and Synthesis of Novel Flavone-Based Histone Deacetylase Inhibitors Antagonizing Activation of STAT3 in Breast Cancer

(2020) Mingming Wei et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight

(2020) Terence C. S. Ho et al.   JOURNAL OF MEDICINAL CHEMISTRY

Characterization of Conformationally Constrained Benzanilide Scaffolds for Potent and Selective HDAC8 Targeting

(2020) Muhammad Murtaza Hassan et al.   JOURNAL OF MEDICINAL CHEMISTRY

Selective Class I HDAC Inhibitors Based on Aryl Ketone Zinc Binding Induce HIV-1 Protein for Clearance

(2020) Jian Liu et al.   ACS Medicinal Chemistry Letters

Development of a selective HDAC inhibitor aimed at reactivating the HIV latent reservoir

(2020) Dane J. Clausen et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

PTG-0861: A novel HDAC6-selective inhibitor as a therapeutic strategy in acute myeloid leukaemia

(2020) Justyna M. Gawel et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Multicomponent Synthesis, Binding Mode, and Structure–Activity Relationship of Selective Histone Deacetylase 6 (HDAC6) Inhibitors with Bifurcated Capping Groups

(2020) Nina Reßing et al.   JOURNAL OF MEDICINAL CHEMISTRY

Rational Design of Suprastat: A Novel Selective Histone Deacetylase 6 Inhibitor with the Ability to Potentiate Immunotherapy in Melanoma Models

(2020) Satish Noonepalle et al.   JOURNAL OF MEDICINAL CHEMISTRY

Spiroindoline-Capped Selective HDAC6 Inhibitors: Design, Synthesis, Structural Analysis, and Biological Evaluation

(2020) A. Prasanth Saraswati et al.   ACS Medicinal Chemistry Letters

Discovery of Highly Selective and Potent HDAC3 Inhibitors Based on a 2-Substituted Benzamide Zinc Binding Group

(2020) Jian Liu et al.   ACS Medicinal Chemistry Letters

Dual inhibitors of histone deacetylases and other cancer-related targets: A pharmacological perspective

(2020) Yuan Gao et al.   BIOCHEMICAL PHARMACOLOGY

Novel Carboline Fungal Histone Deacetylase (HDAC) Inhibitors for Combinational Treatment of Azole-Resistant Candidiasis

(2020) Zhuang Li et al.   JOURNAL OF MEDICINAL CHEMISTRY

Investigation of the in vitro and in vivo efficacy of peptoid-based HDAC inhibitors with dual-stage antiplasmodial activity

(2020) Marcel K.W. Mackwitz et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synergistic induction of apoptosis in resistant head and neck carcinoma and leukemia by alkoxyamide-based histone deacetylase inhibitors

(2020) Leandro A. Alves Avelar et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Novel quinolone-based potent and selective HDAC6 inhibitors: Synthesis, molecular modeling studies and biological investigation

(2020) Nicola Relitti et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Targeting epigenetic modifications in cancer therapy: erasing the roadmap to cancer

(2019) Helai P. Mohammad et al.   NATURE MEDICINE

Development of Multifunctional Histone Deacetylase 6 Degraders with Potent Antimyeloma Activity

(2019) Hao Wu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Bromodomains: a new target class for drug development

(2019) Andrea G. Cochran et al.   NATURE REVIEWS DRUG DISCOVERY

Novel alkoxyamide-based histone deacetylase inhibitors reverse cisplatin resistance in chemoresistant cancer cells

(2019) Yodita Asfaha et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Protective effects of 10,11-dihydro-5H-dibenzo[b,f]azepine hydroxamates on vascular cognitive impairment

(2019) Navdeep Kaur et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Novel 2, 5-diketopiperazine derivatives as potent selective histone deacetylase 6 inhibitors: Rational design, synthesis and antiproliferative activity

(2019) Xin Chen et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and structure activity relationship of 1, 3-benzo-thiazine-2-thiones as selective HDAC8 inhibitors

(2019) Benjamin Wolff et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and in Vitro and in Vivo Biological Evaluation of Tissue-Specific Bisthiazole Histone Deacetylase (HDAC) Inhibitors

(2019) Shu-Wei Zhang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia

(2019) Andrew E. Shouksmith et al.   ACS Medicinal Chemistry Letters

Histone deacetylase 6 in cancer

(2018) Ting Li et al.   Journal of Hematology & Oncology

Beyond histone acetylation—writing and erasing histone acylations

(2018) Shuai Zhao et al.   CURRENT OPINION IN STRUCTURAL BIOLOGY

The Search for Potent, Small-Molecule HDACIs in Cancer Treatment: A Decade After Vorinostat

(2017) Chiara Zagni et al.   MEDICINAL RESEARCH REVIEWS

Chidamide in the treatment of peripheral T-cell lymphoma

(2017) Thomas Chan et al.   OncoTargets and Therapy

Histone deacetylase 10 structure and molecular function as a polyamine deacetylase

(2017) Yang Hai et al.   Nature Communications

HDAC 3-selective inhibitor RGFP966 demonstrates anti-inflammatory properties in RAW 264.7 macrophages and mouse precision-cut lung slices by attenuating NF-κB p65 transcriptional activity

(2016) Niek G.J. Leus et al.   BIOCHEMICAL PHARMACOLOGY

Identification of Histone Deacetylase Inhibitors with Benzoylhydrazide Scaffold that Selectively Inhibit Class I Histone Deacetylases

(2015) Yunfei Wang et al.   CHEMISTRY & BIOLOGY

Why Hydroxamates May Not Be the Best Histone Deacetylase Inhibitors-What Some May Have Forgotten or Would Rather Forget?

(2015) Sida Shen et al.   ChemMedChem

The role dietary of bioactive compounds on the regulation of histone acetylases and deacetylases: A review

(2015) F. Vahid et al.   GENE

Investigations of possible prodrug structures for 2-(2-mercaptophenyl)tetrahydropyrimidines: reductive conversion from anti-HIV agents with pyrimidobenzothiazine and isothiazolopyrimidine scaffolds

(2015) Shiho Okazaki et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

HDAC Family Members Intertwined in the Regulation of Autophagy: A Druggable Vulnerability in Aggressive Tumor Entities

(2015) Emily Koeneke et al.   Cells

Structure and Ligand-Based Design of mTOR and PI3-Kinase Inhibitors Leading to the Clinical Candidates VS-5584 (SB2343) and SB2602

(2014) Anders Poulsen et al.   Journal of Chemical Information and Modeling

Structure of the DDB1–CRBN E3 ubiquitin ligase in complex with thalidomide

(2014) Eric S. Fischer et al.   NATURE

Potent and Orally Efficacious Bisthiazole-Based Histone Deacetylase Inhibitors

(2014) Fei Chen et al.   ACS Medicinal Chemistry Letters

The physiological roles of histone deacetylase (HDAC) 1 and 2: complex co-stars with multiple leading parts

(2013) Richard D.W. Kelly et al.   BIOCHEMICAL SOCIETY TRANSACTIONS

Systematic identification of Class I HDAC substrates

(2013) T. Li et al.   BRIEFINGS IN BIOINFORMATICS

Hopx and Hdac2 Interact to Modulate Gata4 Acetylation and Embryonic Cardiac Myocyte Proliferation

(2010) Chinmay M. Trivedi et al.   DEVELOPMENTAL CELL