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

Safety and Tolerability of Phosphatidylinositol-3-Kinase (PI3K) Inhibitors in Oncology

(2019) Giuseppe Curigliano et al.   DRUG SAFETY

Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 (HDAC6) Inhibitors

(2019) Katharina Vögerl et al.   JOURNAL OF MEDICINAL CHEMISTRY

Targeting PI3K in cancer: mechanisms and advances in clinical trials

(2019) Jing Yang et al.   Molecular Cancer

Selective pharmacological inhibitors of HDAC6 reveal biochemical activity but functional tolerance in cancer models

(2019) Yves Depetter et al.   INTERNATIONAL JOURNAL OF CANCER

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

Entropy as a Driver of Selectivity for Inhibitor Binding to Histone Deacetylase 6

(2018) Nicholas J. Porter et al.   BIOCHEMISTRY

N -Acylhydrazones as drugs

(2018) Sreekanth Thota et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma

(2018) Dizhong Chen 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

Multicomponent Synthesis and Binding Mode of Imidazo[1,2-a]pyridine-Capped Selective HDAC6 Inhibitors

(2018) Marcel K. W. Mackwitz et al.   ORGANIC LETTERS

Modeling zinc-oxygen coordination in histone deacetylase: A comparison of semiempirical methods performance

(2018) Pedro de Sena Murteira Pinheiro et al.   INTERNATIONAL JOURNAL OF QUANTUM CHEMISTRY

Histone Deacetylase 6-Selective Inhibitors and the Influence of Capping Groups on Hydroxamate-Zinc Denticity

(2018) Nicholas J. Porter et al.   JOURNAL OF MEDICINAL CHEMISTRY

Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy

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

Quinazolin-2,4-dione-Based Hydroxamic Acids as Selective Histone Deacetylase-6 Inhibitors for Treatment of Non-Small Cell Lung Cancer

(2018) Chao-Wu Yu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Unusual zinc-binding mode of HDAC6-selective hydroxamate inhibitors

(2017) Nicholas J. Porter et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Inhibitors of histone deacetylase as antitumor agents: A critical review

(2016) Mohammed Manal et al.   BIOORGANIC CHEMISTRY

Multitarget Drugs: an Epigenetic Epiphany

(2016) A. Ganesan   ChemMedChem

Determining Partition Coefficient (Log P), Distribution Coefficient (Log D) and Ionization Constant (pKa) in Early Drug Discovery

(2016) Sonali S. Bharate et al.   COMBINATORIAL CHEMISTRY & HIGH THROUGHPUT SCREENING

Design, Synthesis, and Pharmacological Evaluation of Novel N-Acylhydrazone Derivatives as Potent Histone Deacetylase 6/8 Dual Inhibitors

(2016) Daniel A. Rodrigues 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

Beyond the Selective Inhibition of Histone Deacetylase 6

(2016) Daniel A. Rodrigues et al.   MINI-REVIEWS IN MEDICINAL CHEMISTRY

Histone deacetylase 6 structure and molecular basis of catalysis and inhibition

(2016) Yang Hai et al.   Nature Chemical Biology

Structural insights into HDAC6 tubulin deacetylation and its selective inhibition

(2016) Yasuyuki Miyake et al.   Nature Chemical Biology

AKT activation controls cell survival in response to HDAC6 inhibition

(2016) M Kaliszczak et al.   Cell Death & Disease

Epigenetic polypharmacology: from combination therapy to multitargeted drugs

(2016) Angel R. de Lera et al.   Clinical Epigenetics

Phosphatidylinositol 3-Kinase (PI3K) and Phosphatidylinositol 3-Kinase-Related Kinase (PIKK) Inhibitors: Importance of the Morpholine Ring

(2014) Martin Andrs et al.   JOURNAL OF MEDICINAL CHEMISTRY

Histone deacetylases and their inhibitors in cancer, neurological diseases and immune disorders

(2014) Katrina J. Falkenberg et al.   NATURE REVIEWS DRUG DISCOVERY

Docking, Synthesis and Antiproliferative Activity of N-Acylhydrazone Derivatives Designed as Combretastatin A4 Analogues

(2014) Daniel Nascimento do Amaral et al.   PLoS One

Development and Therapeutic Implications of Selective Histone Deacetylase 6 Inhibitors

(2013) Jay H. Kalin et al.   JOURNAL OF MEDICINAL CHEMISTRY

Polypharmacology – Foe or Friend?

(2013) Jens-Uwe Peters   JOURNAL OF MEDICINAL CHEMISTRY

Crystal Structures of PI3Kα Complexed with PI103 and Its Derivatives: New Directions for Inhibitors Design

(2013) Yanlong Zhao et al.   ACS Medicinal Chemistry Letters

Preclinical activity, pharmacodynamic, and pharmacokinetic properties of a selective HDAC6 inhibitor, ACY-1215, in combination with bortezomib in multiple myeloma

(2012) L. Santo et al.   BLOOD

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

Design, Synthesis, and Pharmacological Evaluation of N-Acylhydrazones and Novel Conformationally Constrained Compounds as Selective and Potent Orally Active Phosphodiesterase-4 Inhibitors

(2012) Arthur E. Kümmerle et al.   JOURNAL OF MEDICINAL CHEMISTRY

Optimization of parameters for semiempirical methods VI: more modifications to the NDDO approximations and re-optimization of parameters

(2012) James J. P. Stewart   JOURNAL OF MOLECULAR MODELING

Improvement in Aqueous Solubility in Small Molecule Drug Discovery Programs by Disruption of Molecular Planarity and Symmetry

(2011) Minoru Ishikawa et al.   JOURNAL OF MEDICINAL CHEMISTRY

Vorinostat interferes with the signaling transduction pathway of T-cell receptor and synergizes with phosphoinositide-3 kinase inhibitors in cutaneous T-cell lymphoma

(2010) M. B. Wozniak et al.   HAEMATOLOGICA

Improving Tenoxicam Solubility and Bioavailability by Cosolvent System

(2009) Ming-Kung Yeh et al.   AAPS PHARMSCITECH

HDAC family: What are the cancer relevant targets?

(2008) Olaf Witt et al.   CANCER LETTERS

The Identification of 2-(1H-Indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a Potent, Selective, Orally Bioavailable Inhibitor of Class I PI3 Kinase for the Treatment of Cancer†

(2008) Adrian J. Folkes et al.   JOURNAL OF MEDICINAL CHEMISTRY

Rapid solubility determination of the triterpenes oleanolic acid and ursolic acid by UV-spectroscopy in different solvents

(2008) P. Schneider et al.   Phytochemistry Letters