Anticancer properties of chimeric HDAC and kinase inhibitors

Design, Synthesis, and Pharmacological Evaluation of First‐in‐Class Multitarget N ‐Acylhydrazone Derivatives as Selective HDAC6/8 and PI3Kα Inhibitors

(2020) Daniel A. Rodrigues et al.   ChemMedChem

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 Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors

(2020) Ashish Thakur et al.   JOURNAL OF MEDICINAL CHEMISTRY

Multitarget Anticancer Agents Based on Histone Deacetylase and Protein Kinase CK2 Inhibitors

(2020) Regina Martínez et al.   MOLECULES

New Dual CK2/HDAC1 Inhibitors with Nanomolar Inhibitory Activity against Both Enzymes

(2020) Loganathan Rangasamy et al.   ACS Medicinal Chemistry Letters

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

Design, Synthesis, and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases

(2019) Kehui Zhang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of novel 9H-purin derivatives as dual inhibitors of HDAC1 and CDK2

(2019) Yu Yu et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of novel phenoxybenzamide analogues as Raf/HDAC dual inhibitors

(2019) Aixin Geng et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Comparison of Radiosensitization by HDAC Inhibitors CUDC-101 and SAHA in Pancreatic Cancer Cells

(2019) Simone Moertl et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Role of protein kinase CK2 in antitumor drug resistance

(2019) Christian Borgo et al.   JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH

Design, Synthesis and Biological Evaluation of Novel Osimertinib-Based HDAC and EGFR Dual Inhibitors

(2019) Hang Dong et al.   MOLECULES

Fibroblast Growth Factor Receptors (FGFRs): Structures and Small Molecule Inhibitors

(2019) Shuyan Dai et al.   Cells

Design, Synthesis and Biological Evaluation of Novel Benzoylimidazole Derivatives as Raf and Histone Deacetylases Dual Inhibitors

(2019) Xin Chen et al.   CHEMICAL & PHARMACEUTICAL BULLETIN

Src Tyrosine Kinase Inhibitors: New Perspectives on Their Immune, Antiviral, and Senotherapeutic Potential

(2019) José Rivera-Torres et al.   Frontiers in Pharmacology

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

Antitumor and antiangiogenic activity of the novel chimeric inhibitor animacroxam in testicular germ cell cancer

(2019) Gustav Steinemann et al.   Molecular Oncology

Design, synthesis and evaluate of novel dual FGFR1 and HDAC inhibitors bearing an indazole scaffold

(2018) Jian Liu et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Design and synthesis of triple inhibitors of janus kinase (JAK), histone deacetylase (HDAC) and Heat Shock Protein 90 (HSP90)

(2018) Lianbin Yao et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

Chimeric HDAC inhibitors: Comprehensive review on the HDAC-based strategies developed to combat cancer

(2018) Heba M. Hesham et al.   MEDICINAL RESEARCH REVIEWS

Function of the c-Met receptor tyrosine kinase in carcinogenesis and associated therapeutic opportunities

(2018) Yazhuo Zhang et al.   Molecular Cancer

CUDC-907 displays potent antitumor activity against human pancreatic adenocarcinoma in vitro and in vivo through inhibition of HDAC6 to downregulate c-Myc expression

(2018) Xu-hong Fu et al.   ACTA PHARMACOLOGICA SINICA

Design and synthesis of potent dual inhibitors of JAK2 and HDAC based on fusing the pharmacophores of XL019 and vorinostat

(2018) Yu-yi Chu-Farseeva et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

A comprehensive review of protein kinase inhibitors for cancer therapy

(2018) Radhamani Kannaiyan et al.   Expert Review of Anticancer Therapy

Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy

(2018) Yepeng Luan et al.   JOURNAL OF MEDICINAL CHEMISTRY

Recent updates on third generation EGFR inhibitors and emergence of fourth generation EGFR inhibitors to combat C797S resistance

(2017) Harun Patel et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Designing multi-targeted agents: An emerging anticancer drug discovery paradigm

(2017) Rong-geng Fu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Histone Deacetylase Inhibitors as Anticancer Drugs

(2017) Tomas Eckschlager et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

CUDC-907, a dual HDAC and PI3K inhibitor, reverses platinum drug resistance

(2017) Kenneth K. W. To et al.   INVESTIGATIONAL NEW DRUGS

Design and Synthesis of Ligand Efficient Dual Inhibitors of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Based on Ruxolitinib and Vorinostat

(2017) Lianbin Yao et al.   JOURNAL OF MEDICINAL CHEMISTRY

Sorafenib: A Review in Hepatocellular Carcinoma

(2017) Gillian M. Keating   Targeted Oncology

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

Design, synthesis and biological evaluation of 2,3-dihydroimidazo[1,2-c]quinazoline derivatives as novel phosphatidylinositol 3-kinase and histone deacetylase dual inhibitors

(2017) Yichao Wu et al.   RSC Advances

Romidepsin for the treatment of relapsed/refractory cutaneous T-cell lymphoma (mycosis fungoides/Sézary syndrome): Use in a community setting

(2016) Sunil A. Reddy   CRITICAL REVIEWS IN ONCOLOGY HEMATOLOGY

Treatment of advanced thyroid cancer with targeted therapies: ten years of experience

(2016) David Viola et al.   ENDOCRINE-RELATED CANCER

An overview of molecular hybrids in drug discovery

(2016) Gervais Bérubé   Expert Opinion on Drug Discovery

Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities

(2016) Yong Chen et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design and Synthesis of Janus Kinase 2 (JAK2) and Histone Deacetlyase (HDAC) Bispecific Inhibitors Based on Pacritinib and Evidence of Dual Pathway Inhibition in Hematological Cell Lines

(2016) Eugene Guorong Yang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Safety, tolerability, and preliminary activity of CUDC-907, a first-in-class, oral, dual inhibitor of HDAC and PI3K, in patients with relapsed or refractory lymphoma or multiple myeloma: an open-label, dose-escalation, phase 1 trial

(2016) Anas Younes et al.   LANCET ONCOLOGY

Dual HDAC and PI3K Inhibitor CUDC-907 Downregulates MYC and Suppresses Growth of MYC-dependent Cancers

(2016) Kaiming Sun et al.   MOLECULAR CANCER THERAPEUTICS

Drug priming enhances radiosensitivity of adamantinomatous craniopharyngioma via downregulation of survivin

(2016) Christina Stache et al.   Neurosurgical Focus

A Review of Ruxolitinib for the Treatment of Myelofibrosis: A Critique of the Evidence

(2016) Ros Wade et al.   PHARMACOECONOMICS

Carfilzomib potentiates CUDC-101-induced apoptosis in anaplastic thyroid cancer

(2016) Lisa Zhang et al.   Oncotarget

CUDC-101, a Novel Inhibitor of Full-Length Androgen Receptor (flAR) and Androgen Receptor Variant 7 (AR-V7) Activity: Mechanism of Action and In Vivo Efficacy

(2016) Huiying Sun et al.   Hormones & Cancer

Hybrids from 4-anilinoquinazoline and hydroxamic acid as dual inhibitors of vascular endothelial growth factor receptor-2 and histone deacetylase

(2015) Fan-Wei Peng et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Biochemical, biological and structural properties of romidepsin (FK228) and its analogs as novel HDAC/PI3K dual inhibitors

(2015) Ken Saijo et al.   CANCER SCIENCE

A Phase I Study of CUDC-101, a Multitarget Inhibitor of HDACs, EGFR, and HER2, in Combination with Chemoradiation in Patients with Head and Neck Squamous Cell Carcinoma

(2015) T. J. Galloway et al.   CLINICAL CANCER RESEARCH

Panobinostat: First Global Approval

(2015) Karly P. Garnock-Jones   DRUGS

Macrocyclic compounds as anti-cancer agents: Design and synthesis of multi-acting inhibitors against HDAC, FLT3 and JAK2

(2015) Cheng-Qing Ning et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Histone Deacetylase Inhibitors in Clinical Studies as Templates for New Anticancer Agents

(2015) Madhusoodanan Mottamal et al.   MOLECULES

HDAC Inhibitors as Novel Anti-Cancer Therapeutics

(2015) Cristabelle Souza et al.   Recent Patents on Anti-Cancer Drug Discovery

Histone Deacetylase Inhibitors Resensitize EGFR/EGFRvIII-Overexpressing, Erlotinib-Resistant Glioblastoma Cells to Tyrosine Kinase Inhibition

(2015) Katrin Liffers et al.   Targeted Oncology

Dual inhibition of HDAC and EGFR signaling with CUDC-101 induces potent suppression of tumor growth and metastasis in anaplastic thyroid cancer

(2015) Lisa Zhang et al.   Oncotarget

Design, synthesis and biological evaluation of 4-anilinothieno[2,3-d]pyrimidine-based hydroxamic acid derivatives as novel histone deacetylase inhibitors

(2014) Wei Yang et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Phase I First-in-Human Study of CUDC-101, a Multitargeted Inhibitor of HDACs, EGFR, and HER2 in Patients with Advanced Solid Tumors

(2014) T. Shimizu et al.   CLINICAL CANCER RESEARCH

Belinostat: First Global Approval

(2014) Raewyn M. Poole   DRUGS

Discovery of a Potent and Selective EGFR Inhibitor (AZD9291) of Both Sensitizing and T790M Resistance Mutations That Spares the Wild Type Form of the Receptor

(2014) M. Raymond V. Finlay et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis of hybrid anticancer agents based on kinase and histone deacetylase inhibitors

(2014) Hiren Patel et al.   MedChemComm

JAK Inhibitors: Pharmacology and Clinical Activity in Chronic Myeloprolipherative Neoplasms

(2013) J. Trelinski et al.   CURRENT MEDICINAL CHEMISTRY

Combination of a novel HDAC inhibitor OBP-801/YM753 and a PI3K inhibitor LY294002 synergistically induces apoptosis in human endometrial carcinoma cells due to increase of Bim with accumulation of ROS

(2013) Takashi Yoshioka et al.   GYNECOLOGIC ONCOLOGY

A novel HDAC inhibitor OBP-801 and a PI3K inhibitor LY294002 synergistically induce apoptosis via the suppression of survivin and XIAP in renal cell carcinoma

(2013) TAKESHI YAMADA et al.   INTERNATIONAL JOURNAL OF ONCOLOGY

Potential Advantages of CUDC-101, a Multitargeted HDAC, EGFR, and HER2 Inhibitor, in Treating Drug Resistance and Preventing Cancer Cell Migration and Invasion

(2013) J. Wang et al.   MOLECULAR CANCER THERAPEUTICS

The Design and Synthesis of a New Class of RTK/HDAC Dual-Targeted Inhibitors

(2013) Xuan Zhang et al.   MOLECULES

Development of a Chimeric c-Src Kinase and HDAC Inhibitor

(2013) Kristin S. Ko et al.   ACS Medicinal Chemistry Letters

Synthesis and biological evaluation of N-aryl salicylamides with a hydroxamic acid moiety at 5-position as novel HDAC–EGFR dual inhibitors

(2012) Miao Zuo et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Romidepsin (FK228) and its analogs directly inhibit phosphatidylinositol 3-kinase activity and potently induce apoptosis as histone deacetylase/phosphatidylinositol 3-kinase dual inhibitors

(2012) Ken Saijo et al.   CANCER SCIENCE

Cancer Network Disruption by a Single Molecule Inhibitor Targeting Both Histone Deacetylase Activity and Phosphatidylinositol 3-Kinase Signaling

(2012) C. Qian et al.   CLINICAL CANCER RESEARCH

Trials with ‘epigenetic’ drugs: An update

(2012) Angela Nebbioso et al.   Molecular Oncology

ARAF acts as a scaffold to stabilize BRAF:CRAF heterodimers

(2012) A P Rebocho et al.   ONCOGENE

Histone Deacetylase Inhibitors Induce Epithelial-to-Mesenchymal Transition in Prostate Cancer Cells

(2012) Dejuan Kong et al.   PLoS One

CUDC-101, a Multitargeted Inhibitor of Histone Deacetylase, Epidermal Growth Factor Receptor, and Human Epidermal Growth Factor Receptor 2, Exerts Potent Anticancer Activity

(2010) Cheng-Jung Lai et al.   CANCER RESEARCH

Discovery of 7-(4-(3-Ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDC-101) as a Potent Multi-Acting HDAC, EGFR, and HER2 Inhibitor for the Treatment of Cancer

(2010) Xiong Cai et al.   JOURNAL OF MEDICINAL CHEMISTRY

Novel Chimeric Histone Deacetylase Inhibitors: A Series of Lapatinib Hybrides as Potent Inhibitors of Epidermal Growth Factor Receptor (EGFR), Human Epidermal Growth Factor Receptor 2 (HER2), and Histone Deacetylase Activity

(2010) Siavosh Mahboobi et al.   JOURNAL OF MEDICINAL CHEMISTRY

New Protein Kinase CK2 Inhibitors: Jumping out of the Catalytic Box

(2009) Renaud Prudent et al.   CHEMISTRY & BIOLOGY

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

Protein Kinase CK2 in Human Diseases

(2008) Barbara Guerra et al.   CURRENT MEDICINAL CHEMISTRY

The ErbB kinase domain: Structural perspectives into kinase activation and inhibition

(2008) Ron Bose et al.   EXPERIMENTAL CELL RESEARCH

Histone Deacetylase Inhibitors: From Bench to Clinic

(2008) Marielle Paris et al.   JOURNAL OF MEDICINAL CHEMISTRY