A review of progress in o-aminobenzamide-based HDAC inhibitors with dual targeting capabilities for cancer therapy

Entinostat-Bortezomib Hybrids against Multiple Myeloma

(2023) Angelica Ferro et al.   MOLECULES

Recent development of multi-target VEGFR-2 inhibitors for the cancer therapy

(2023) Xiu-Juan Liu et al.   BIOORGANIC CHEMISTRY

Discovery of novel tranylcypromine-based derivatives as LSD1 inhibitors for gastric cancer treatment

(2023) Qi-Sheng Ma et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of novel and bioavailable histone deacetylases and cyclin-dependent kinases dual inhibitor to impair the stemness of leukemia cells

(2023) Yulin Liu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of novel N-benzylarylamide-dithiocarbamate based derivatives as dual inhibitors of tubulin polymerization and LSD1 that inhibit gastric cancers

(2023) Xin-Ying Yuan et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

New drug approvals for 2022: Synthesis and clinical applications

(2023) Shuo Yuan et al.   MEDICINAL RESEARCH REVIEWS

Discovery of DNA-Targeting HDAC Inhibitors with Potent Antitumor Efficacy In Vivo That Trigger Antitumor Immunity

(2022) Chen Chen et al.   JOURNAL OF MEDICINAL CHEMISTRY

HDAC Inhibitors: Innovative Strategies for Their Design and Applications

(2022) Mateusz Daśko et al.   MOLECULES

2-Methoxydiol derivatives as new tubulin and HDAC dual-targeting inhibitors, displaying antitumor and antiangiogenic response

(2022) Moran Sun et al.   BIOORGANIC CHEMISTRY

Design, Synthesis, and Structure-Activity relationships of Evodiamine-Based topoisomerase (Top)/Histone deacetylase (HDAC) dual inhibitors

(2022) Fugui Zhu et al.   BIOORGANIC CHEMISTRY

Dual-acting antitumor agents targeting the A2A adenosine receptor and histone deacetylases: Design and synthesis of 4-(furan-2-yl)-1H-pyrazolo[3,4-d]pyrimidin-6-amine derivatives

(2022) Jinfeng Zhang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Estrogen Receptor Complex to Trigger or Delay Estrogen-Induced Apoptosis in Long-Term Estrogen Deprived Breast Cancer

(2022) Philipp Y. Maximov et al.   Frontiers in Endocrinology

A novel aromatic amide derivative SY-65 co-targeted tubulin and histone deacetylase 1 with potent anticancer activity in vitro and in vivo

(2022) Yin-Ru Li et al.   BIOCHEMICAL PHARMACOLOGY

Discovery of novel coumarin-indole derivatives as tubulin polymerization inhibitors with potent anti-gastric cancer activities

(2022) Jian Song et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design and synthesis of highly TRAIL expression HDAC inhibitors based on ONC201 to promote apoptosis of colorectal cancer

(2022) Hao Cui et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

A Perspective Study on the RTK, PI3K, B‐Raf, CDK and the Multi‐Protein Targeting in Medicinal Chemistry

(2022) Abdalla R. Mohamed et al.   CHEMISTRY & BIODIVERSITY

Discovery of N-benzylarylamide derivatives as novel tubulin polymerization inhibitors capable of activating the Hippo pathway

(2022) Jian Song et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

The emerging roles of HDACs and their therapeutic implications in cancer

(2022) Rihan Hai et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Design, synthesis and biological evaluation of 2,4-pyrimidinediamine derivatives as ALK and HDACs dual inhibitors for the treatment of ALK addicted cancer

(2022) Dafeng Guo et al.   JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY

Current trends in development of HDAC-based chemotherapeutics

(2022) Narges Cheshmazar et al.   LIFE SCIENCES

Can We Efficiently Target HDAC in Cancer?

(2022) Tobias Kiesslich et al.   Cancers

The dual FAK-HDAC inhibitor MY-1259 displays potent activities in gastric cancers in vitro and in vivo

(2022) Jian Song et al.   BIOORGANIC CHEMISTRY

New drug approvals for 2021: Synthesis and clinical applications

(2022) Shuo Yuan et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Inhibition of FGF‐FGFR and VEGF‐VEGFR signalling in cancer treatment

(2021) Guihong Liu et al.   CELL PROLIFERATION

A Review of Progress in Histone Deacetylase 6 Inhibitors Research: Structural Specificity and Functional Diversity

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

Oncogenic functions and therapeutic targeting of EphA2 in cancer

(2021) Kalin Wilson et al.   ONCOGENE

New drug approvals for 2020: Synthesis and clinical applications

(2021) Shuo Yuan et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

CAP rigidification of MS-275 and chidamide leads to enhanced antiproliferative effects mediated through HDAC1, 2 and tubulin polymerization inhibition

(2021) Arshdeep Singh et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Traditional Chinese medicines and their active ingredients sensitize cancer cells to TRAIL-induced apoptosis

(2021) Bingyu Sun et al.   Journal of Zhejiang University-SCIENCE B

The HDAC1 Inhibitor CBUD-1001 Enhances TRAIL-induced Apoptosis in Colorectal Cancer Cells

(2021) MIN WOO SHIN et al.   ANTICANCER RESEARCH

Revisiting Nitric Oxide Signaling: Where Was It, and Where Is It Going?

(2021) Michael A. Marletta   BIOCHEMISTRY

Anticancer Activity and Mechanisms of Action of New Chimeric EGFR/HDAC-Inhibitors

(2021) Nils Goehringer et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Efficient Synthesis and Bioevaluation of Novel Dual Tubulin/Histone Deacetylase 3 Inhibitors as Potential Anticancer Agents

(2021) Xiaopeng Peng et al.   JOURNAL OF MEDICINAL CHEMISTRY

Rational Multitargeted Drug Design Strategy from the Perspective of a Medicinal Chemist

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

Recent Progress on Tubulin Inhibitors with Dual Targeting Capabilities for Cancer Therapy

(2021) Wen Shuai et al.   JOURNAL OF MEDICINAL CHEMISTRY

Drug Discovery Targeting Focal Adhesion Kinase (FAK) as a Promising Cancer Therapy

(2021) Xiao-Jing Pang et al.   MOLECULES

Protective Effects of Estrogen on Cardiovascular Disease Mediated by Oxidative Stress

(2021) Du Xiang et al.   Oxidative Medicine and Cellular Longevity

HDAC Screening Identifies the HDAC Class I Inhibitor Romidepsin as a Promising Epigenetic Drug for Biliary Tract Cancer

(2021) Christian Mayr et al.   Cancers

Dual-function antiandrogen/HDACi hybrids based on enzalutamide and entinostat

(2021) Ryan R.G. Barrett et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

HDAC/MIF dual inhibitor inhibits NSCLC cell survival and proliferation by blocking the AKT pathway

(2021) Fangyuan Cao et al.   BIOORGANIC CHEMISTRY

Discovery of 2,4-pyrimidinediamine derivatives as potent dual inhibitors of ALK and HDAC

(2021) Tao Pan et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design, synthesis and biological evaluation of novel o-aminobenzamide derivatives as potential anti-gastric cancer agents in vitro and in vivo

(2021) Yiyue Feng et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of novel tubulin/HDAC dual-targeting inhibitors with strong antitumor and antiangiogenic potency

(2021) Yingge Wang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Molecular hybrids: A five-year survey on structures of multiple targeted hybrids of protein kinase inhibitors for cancer therapy

(2021) Osama M. Soltan et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design, synthesis and evaluation of novel bis-substituted aromatic amide dithiocarbamate derivatives as colchicine site tubulin polymerization inhibitors with potent anticancer activities

(2021) Ya-Xin Sun et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Research progress of dual inhibitors targeting crosstalk between histone epigenetic modulators for cancer therapy

(2021) Ying-Chao Duan et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design and synthesis of dual inhibitors targeting snail and histone deacetylase for the treatment of solid tumour cancer

(2021) Hao Cui et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design and synthesis of HDAC inhibitors to enhance the therapeutic effect of diffuse large B-cell lymphoma by improving metabolic stability and pharmacokinetic characteristics

(2021) Hao Cui et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

A first-in-class anticancer dual HDAC2/FAK inhibitors bearing hydroxamates/benzamides capped by pyridinyl-1,2,4-triazoles

(2021) Muhamad Mustafa et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis, Molecular Docking and Biological Characterization of Pyrazine Linked 2-Aminobenzamides as New Class I Selective Histone Deacetylase (HDAC) Inhibitors with Anti-Leukemic Activity

(2021) Hany S. Ibrahim et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Structure-Based Design of Dual-Acting Compounds Targeting Adenosine A2A Receptor and Histone Deacetylase as Novel Tumor Immunotherapeutic Agents

(2021) Wenzhong Yan et al.   JOURNAL OF MEDICINAL CHEMISTRY

HDAC inhibitors: Targets for tumor therapy, immune modulation and lung diseases

(2021) Geetha Shanmugam et al.   Translational Oncology

Design, synthesis and anticancer activities of novel dual poly(ADP-ribose) polymerase-1/histone deacetylase-1 inhibitors

(2020) Yongbin Tian et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of novel cyclin-dependent kinase (CDK) and histone deacetylase (HDAC) dual inhibitors with potent in vitro and in vivo anticancer activity

(2020) Chunhui Cheng et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design, synthesis, and evaluation of N-phenyl-4-(2-phenylsulfonamido)-benzamides as microtubule-targeting agents in drug-resistant cancer cells, displaying HDAC inhibitory response

(2020) Wei-Cheng Wu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

The novel dual BET/HDAC inhibitor TW09 mediates cell death by mitochondrial apoptosis in rhabdomyosarcoma cells

(2020) Stephanie Laszig et al.   CANCER LETTERS

Dual-Target Inhibitors Based on HDACs: Novel Antitumor Agents for Cancer Therapy

(2020) Tingting Liu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Peptide Boronate Derivatives as Histone Deacetylase and Proteasome Dual Inhibitors for Overcoming Bortezomib Resistance of Multiple Myeloma

(2020) Yi Zhou et al.   JOURNAL OF MEDICINAL CHEMISTRY

Less-well known functions of cyclin/CDK complexes

(2020) Nathan Palmer et al.   SEMINARS IN CELL & DEVELOPMENTAL BIOLOGY

Recent Advances in NAMPT Inhibitors: A Novel Immunotherapic Strategy

(2020) Ubaldina Galli et al.   Frontiers in Pharmacology

CUDC-907 enhances TRAIL-induced apoptosis through upregulation of DR5 in breast cancer cells

(2020) Zhao-Jun Li et al.   Journal of Cell Communication and Signaling

Discovery of novel dual c-Met/HDAC inhibitors as a promising strategy for cancer therapy

(2020) Hao Hu et al.   BIOORGANIC CHEMISTRY

Design, synthesis and biological evaluation of novel histone deacetylase1/2 (HDAC1/2) and cyclin-dependent Kinase2 (CDK2) dual inhibitors against malignant cancer

(2020) Fan Yun 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

Paradigm Shift of “Classical” HDAC Inhibitors to “Hybrid” HDAC inhibitors in Therapeutic Interventions

(2020) Gargi Nikhil Vaidya et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of selective HDAC/BRD4 dual inhibitors as epigenetic probes

(2020) Jingjing Chen et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of tertiary amide derivatives incorporating benzothiazole moiety as anti-gastric cancer agents in vitro via inhibiting tubulin polymerization and activating the Hippo signaling pathway

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

Discovery of Novel Indoleamine 2,3-Dioxygenase 1 (IDO1) and Histone Deacetylase 1 (HDAC1) Dual Inhibitors Derived from the Natural Product Saprorthoquinone

(2020) Yang Lin et al.   MOLECULES

USP29 enhances chemotherapy-induced stemness in non-small cell lung cancer via stabilizing Snail1 in response to oxidative stress

(2020) Yueguang Wu et al.   Cell Death & Disease

Tumor Immunotherapy Using A2A Adenosine Receptor Antagonists

(2020) Jinfeng Zhang et al.   Pharmaceuticals

MIF-Dependent Control of Tumor Immunity

(2020) Jordan T. Noe et al.   Frontiers in Immunology

Anticancer properties of chimeric HDAC and kinase inhibitors

(2020) Bernhard Biersack et al.   SEMINARS IN CANCER BIOLOGY

Elucidating the mechanism of action of domatinostat (4SC-202) in cutaneous T cell lymphoma cells

(2019) Marion Wobser et al.   Journal of Hematology & Oncology

Development of a Potent Protein Degrader against Oncogenic BCR-ABL Protein

(2019) Norihito Shibata et al.   CHEMICAL & PHARMACEUTICAL BULLETIN

Macrophage migration inhibitory factor (MIF) as a therapeutic target for rheumatoid arthritis and systemic lupus erythematosus

(2019) Joshua B. Bilsborrow et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

A Synergistic Anti-Cancer FAK and HDAC Inhibitor Combination Discovered by a Novel Chemical-Genetic High-Content Phenotypic Screen

(2019) John C Dawson et al.   MOLECULAR CANCER THERAPEUTICS

Cell Cycle-Dependent Control and Roles of DNA Topoisomerase II

(2019) Joyce H. Lee et al.   Genes

Domatinostat favors the immunotherapy response by modulating the tumor immune microenvironment (TIME)

(2019) Anne Catherine Bretz et al.   Journal for ImmunoTherapy of Cancer

Evodiamine-inspired dual inhibitors of histone deacetylase 1 (HDAC1) and topoisomerase 2 (TOP2) with potent antitumor activity

(2019) Yahui Huang et al.   Acta Pharmaceutica Sinica B

LSD1/KDM1A inhibitors in clinical trials: advances and prospects

(2019) Yuan Fang et al.   Journal of Hematology & Oncology

Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties

(2019) Viktoria Krieger et al.   JOURNAL OF MEDICINAL CHEMISTRY

Nicotinamide Phosphoribosyltransferase (NAMPT) Is a New Target of Antitumor Agent Chidamide

(2019) Ying Wu et al.   ACS Medicinal Chemistry Letters

Topoisomerases as anticancer targets

(2018) Justine L. Delgado et al.   BIOCHEMICAL JOURNAL

Developing TRAIL/TRAIL death receptor-based cancer therapies

(2018) Xun Yuan et al.   CANCER AND METASTASIS REVIEWS

Inhibition of the adenosine A2a receptor modulates expression of T cell coinhibitory receptors and improves effector function for enhanced checkpoint blockade and ACT in murine cancer models

(2018) Robert D. Leone et al.   CANCER IMMUNOLOGY IMMUNOTHERAPY

IDO1 in cancer: a Gemini of immune checkpoints

(2018) Lijie Zhai et al.   Cellular & Molecular Immunology

Structural and biological characterization of new hybrid drugs joining an HDAC inhibitor to different NO-donors

(2018) Sandra Atlante et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously

(2018) Jie Zang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Recent Developments in Drug Design of NO-donor Hybrid Compounds

(2018) Rajan Sharma et al.   MINI-REVIEWS IN MEDICINAL CHEMISTRY

The function and therapeutic targeting of anaplastic lymphoma kinase (ALK) in non-small cell lung cancer (NSCLC)

(2018) Brandon Golding et al.   Molecular Cancer

Combination Therapies Targeting HDAC and IKK in Solid Tumors

(2018) Ivana Vancurova et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Discovery of Novel Indoleamine 2,3-Dioxygenase 1 (IDO1) and Histone Deacetylase (HDAC) Dual Inhibitors

(2018) Kun Fang et al.   ACS Medicinal Chemistry Letters

Pathogenic role for macrophage migration inhibitory factor in glioblastoma and its targeting with specific inhibitors as novel tailored therapeutic approach

(2018) Katia Mangano et al.   Oncotarget

HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors

(2018) Rekha Sangwan et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Hybrid topoisomerase I and HDAC inhibitors as dual action anticancer agents

(2018) Raffaella Cincinelli et al.   PLoS One

1-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase

(2018) Mei-Jung Lai et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Targeting adenosine A2A receptor antagonism for treatment of cancer

(2018) Miles Congreve et al.   Expert Opinion on Drug Discovery

Design and synthesis of tranylcypromine derivatives as novel LSD1/HDACs dual inhibitors for cancer treatment

(2017) Ying-Chao Duan et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

IDO1: An important immunotherapy target in cancer treatment

(2017) Fangxuan Li et al.   INTERNATIONAL IMMUNOPHARMACOLOGY

Small Molecule Inhibitors Simultaneously Targeting Cancer Metabolism and Epigenetics: Discovery of Novel Nicotinamide Phosphoribosyltransferase (NAMPT) and Histone Deacetylase (HDAC) Dual Inhibitors

(2017) Guoqiang Dong et al.   JOURNAL OF MEDICINAL CHEMISTRY

Nitric Oxide Donor-Based Cancer Therapy: Advances and Prospects

(2017) Zhangjian Huang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Stepwise assembly of functional C-terminal REST/NRSF transcriptional repressor complexes as a drug target

(2017) Ken Inui et al.   PROTEIN SCIENCE

Design, Synthesis, and Biological Evaluation of the First c-Met/HDAC Inhibitors Based on Pyridazinone Derivatives

(2017) Dong Lu et al.   ACS Medicinal Chemistry Letters

Dual NAMPT/HDAC Inhibitors as a New Strategy for Multitargeting Antitumor Drug Discovery

(2017) Wei Chen et al.   ACS Medicinal Chemistry Letters

HDAC inhibitors enhance the immunotherapy response of melanoma cells

(2017) Laurence Booth et al.   Oncotarget

4SC-202 activates ASK1-dependent mitochondrial apoptosis pathway to inhibit hepatocellular carcinoma cells

(2016) Meili Fu et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Synthesis and Biological Evaluation of 1-(2-Aminophenyl)-3-arylurea Derivatives as Potential EphA2 and HDAC Dual Inhibitors

(2016) Yong Zhu et al.   CHEMICAL & PHARMACEUTICAL BULLETIN

An Update on Poly(ADP-ribose)polymerase-1 (PARP-1) Inhibitors: Opportunities and Challenges in Cancer Therapy

(2016) Ying-Qing Wang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Aromatase: Contributions to Physiology and Disease in Women and Men

(2016) Jennifer Blakemore et al.   PHYSIOLOGY

Discovery of selective small-molecule HDAC6 inhibitor for overcoming proteasome inhibitor resistance in multiple myeloma

(2016) Teru Hideshima et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Cancer Stem Cell-Secreted Macrophage Migration Inhibitory Factor Stimulates Myeloid Derived Suppressor Cell Function and Facilitates Glioblastoma Immune Evasion

(2016) Balint Otvos et al.   STEM CELLS

Evaluation of the Therapeutic Potential of the Novel Isotype Specific HDAC Inhibitor 4SC-202 in Urothelial Carcinoma Cell Lines

(2016) Maria Pinkerneil et al.   Targeted Oncology

IDO in the Tumor Microenvironment: Inflammation, Counter-Regulation, and Tolerance

(2016) David H. Munn et al.   TRENDS IN IMMUNOLOGY

Pre-clinical characterization of 4SC-202, a novel class I HDAC inhibitor, against colorectal cancer cells

(2016) Huang Zhijun et al.   TUMOR BIOLOGY

Design, synthesis and evaluation of antiestrogen and histone deacetylase inhibitor molecular hybrids

(2015) Rodrigo Mendoza-Sanchez et al.   BIOORGANIC & MEDICINAL CHEMISTRY

The pan-HDAC inhibitor panobinostat acts as a sensitizer for erlotinib activity in EGFR-mutated and -wildtype non-small cell lung cancer cells

(2015) Gabriele Greve et al.   BMC CANCER

Hologram quantitative structure–activity relationship and comparative molecular interaction field analysis of aminothiazole and thiazolesulfonamide as reversible LSD1 inhibitors

(2015) Vinícius G Maltarollo et al.   Future Medicinal Chemistry

Discovery of novel Bcr-Abl inhibitors with diacylated piperazine as the flexible linker

(2015) Xiaoyan Pan et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Neural Crest Development and Craniofacial Morphogenesis Is Coordinated by Nitric Oxide and Histone Acetylation

(2014) Yawei Kong et al.   CHEMISTRY & BIOLOGY

The Role of Snail in EMT and Tumorigenesis

(2014) Yifan Wang et al.   CURRENT CANCER DRUG TARGETS

Targeting FAK in human cancer: from finding to first clinical trials

(2014) Vita Golubovskaya   Frontiers in Bioscience-Landmark

Improved Synthesis and Structural Reassignment of MC1568: A Class IIa Selective HDAC Inhibitor

(2014) Cassandra L. Fleming et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Mechanisms behind the Therapeutic Activity of BET Bromodomain Inhibition

(2014) Junwei Shi et al.   MOLECULAR CELL

Thiazolocarboxamide Analogues as NAMPT Inhibitors

(2014) Jean-Francois Brazeau et al.   ACS Medicinal Chemistry Letters

The discovery and optimization of novel dual inhibitors of topoisomerase ii and histone deacetylase

(2013) Xuan Zhang et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Cdks, cyclins and CKIs: roles beyond cell cycle regulation

(2013) S. Lim et al.   DEVELOPMENT

Sorafenib and HDAC inhibitors synergize with TRAIL to kill tumor cells

(2013) Hossein A. Hamed et al.   JOURNAL OF CELLULAR PHYSIOLOGY

Medicinal Chemistry of Nicotinamide Phosphoribosyltransferase (NAMPT) Inhibitors

(2013) Ubaldina Galli et al.   JOURNAL OF MEDICINAL CHEMISTRY

Vorinostat or placebo in combination with bortezomib in patients with multiple myeloma (VANTAGE 088): a multicentre, randomised, double-blind study

(2013) Meletios Dimopoulos et al.   LANCET ONCOLOGY

The HDAC inhibitor, MPT0E028, enhances erlotinib-induced cell death in EGFR-TKI-resistant NSCLC cells

(2013) M-C Chen et al.   Cell Death & Disease

Synthesis and Biological Evaluation of the First Example of NO-Donor Histone Deacetylase Inhibitor

(2013) Emily Borretto et al.   ACS Medicinal Chemistry Letters

Combination of HDAC and topoisomerase inhibitors in small cell lung cancer

(2012) Jhanelle Gray et al.   CANCER BIOLOGY & THERAPY

Chimerically designed HDAC- and tyrosine kinase inhibitors. A series of erlotinib hybrids as dual-selective inhibitors of EGFR, HER2 and histone deacetylases

(2012) Thomas Beckers et al.   MedChemComm

Effects of BCR-ABL Inhibitors on Anti-Tumor Immunity

(2011) M. Krusch et al.   CURRENT MEDICINAL CHEMISTRY

The androgen receptor fuels prostate cancer by regulating central metabolism and biosynthesis

(2011) Charles E Massie et al.   EMBO JOURNAL

Structural Basis of Type II Topoisomerase Inhibition by the Anticancer Drug Etoposide

(2011) C.-C. Wu et al.   SCIENCE

Building on bortezomib: second-generation proteasome inhibitors as anti-cancer therapy

(2010) Lawrence R. Dick et al.   DRUG DISCOVERY TODAY

Selective inhibition of BET bromodomains

(2010) Panagis Filippakopoulos et al.   NATURE

Histone Deacetylases Are Required for Androgen Receptor Function in Hormone-Sensitive and Castrate-Resistant Prostate Cancer

(2009) D. S. Welsbie et al.   CANCER RESEARCH

Design of Chimeric Histone Deacetylase- and Tyrosine Kinase-Inhibitors: A Series of Imatinib Hybrides as Potent Inhibitors of Wild-Type and Mutant BCR-ABL, PDGF-Rβ, and Histone Deacetylases†

(2009) Siavosh Mahboobi et al.   JOURNAL OF MEDICINAL CHEMISTRY

HDAC2 blockade by nitric oxide and histone deacetylase inhibitors reveals a common target in Duchenne muscular dystrophy treatment

(2008) C. Colussi et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA