Discovery of benzamide-based PI3K/HDAC dual inhibitors with marked pro-apoptosis activity in lymphoma cells

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

(2023) Wei-Xin Zhang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Umbralisib: First Approval

(2021) Sohita Dhillon et al.   DRUGS

Fimepinostat (CUDC‐907) in patients with relapsed/refractory diffuse large B cell and high‐grade B‐cell lymphoma: report of a phase 2 trial and exploratory biomarker analyses

(2021) Daniel J. Landsburg et al.   BRITISH JOURNAL OF HAEMATOLOGY

Molecular design of dual inhibitors of PI3K and potential molecular target of cancer for its treatment: A review

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

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

CUDC‐907, a novel dual PI3K and HDAC inhibitor, in prostate cancer: Antitumour activity and molecular mechanism of action

(2020) Cheng Hu et al.   JOURNAL OF CELLULAR AND MOLECULAR MEDICINE

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 inhibition of histone deacetylase (HDAC) and phosphatidylinositol‐3‐kinase (PI3K): Current and future prospects

(2020) Carlos Alberto Manssour Fraga et al.   ChemMedChem

Antileukemic activity and mechanism of action of the novel PI3K and histone deacetylase dual inhibitor CUDC-907 in acute myeloid leukemia

(2019) Xinyu Li et al.   HAEMATOLOGICA

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

Alpelisib: First Global Approval

(2019) Anthony Markham   DRUGS

Exploiting polypharmacology for improving therapeutic outcome of kinase inhibitors (KIs): An update of recent medicinal chemistry efforts

(2018) Xiaodong Ma et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

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

Polypharmacology by Design: A Medicinal Chemist’s Perspective on Multitargeting Compounds

(2018) Ewgenij Proschak et al.   JOURNAL OF MEDICINAL CHEMISTRY

Duvelisib: First Global Approval

(2018) Hannah A. Blair   DRUGS

Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy

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

Histone Deacetylase Inhibitors as Anticancer Drugs

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

Isoform-selective inhibitor of histone deacetylase 3 (HDAC3) limits pancreatic islet infiltration and protects female nonobese diabetic mice from diabetes

(2017) Ercument Dirice et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

PI3K/mTOR dual inhibitor BEZ235 and histone deacetylase inhibitor Trichostatin A synergistically exert anti-tumor activity in breast cancer

(2017) Liyan Chen et al.   Oncotarget

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

Multitarget Drug Discovery and Polypharmacology

(2016) Maria Laura Bolognesi et al.   ChemMedChem

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

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

Superior efficacy of co-treatment with the dual PI3K/mTOR inhibitor BEZ235 and histone deacetylase inhibitor Trichostatin A against NSCLC

(2016) Junjie Piao et al.   Oncotarget

PI3K/mTOR Inhibition Markedly Potentiates HDAC Inhibitor Activity in NHL Cells through BIM- and MCL-1-Dependent Mechanisms In Vitro and In Vivo

(2014) M. Rahmani et al.   CLINICAL CANCER RESEARCH

Idelalisib: First Global Approval

(2014) Anthony Markham   DRUGS

Drug–drug interactions with tyrosine-kinase inhibitors: a clinical perspective

(2014) Roelof W F van Leeuwen et al.   LANCET ONCOLOGY

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

Polypharmacology: drug discovery for the future

(2012) A Srinivas Reddy et al.   Expert Review of Clinical Pharmacology

Identification of 2-oxatriazines as highly potent pan-PI3K/mTOR dual inhibitors

(2011) Christoph M. Dehnhardt et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

The PI3K Pathway As Drug Target in Human Cancer

(2010) Kevin D. Courtney et al.   JOURNAL OF CLINICAL ONCOLOGY

Bis(morpholino-1,3,5-triazine) Derivatives: Potent Adenosine 5′-Triphosphate Competitive Phosphatidylinositol-3-kinase/Mammalian Target of Rapamycin Inhibitors: Discovery of Compound26(PKI-587), a Highly Efficacious Dual Inhibitor

(2010) Aranapakam M. Venkatesan et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Emerging Role of the Phosphatidylinositol 3-Kinase/ Akt/Mammalian Target of Rapamycin Signaling Network in Cancer Stem Cell Biology

(2010) Alberto M. Martelli et al.   Cancers

Network pharmacology: the next paradigm in drug discovery

(2008) Andrew L Hopkins   Nature Chemical Biology

Class I PI3K in oncogenic cellular transformation

(2008) L Zhao et al.   ONCOGENE