Precision Deuteration in Search of Anticancer Agents: Approaches to Cancer Drug Discovery

Scalable and selective deuteration of (hetero)arenes

(2022) Wu Li et al.   Nature Chemistry

Deucravacitinib for the Treatment of Psoriatic Disease

(2022) Ana Maria Lé et al.   AMERICAN JOURNAL OF CLINICAL DERMATOLOGY

An Unexpected Deuterium-Induced Metabolic Switch in Doxophylline

(2022) Silvio Aprile et al.   ACS Medicinal Chemistry Letters

Deucravacitinib: First Approval

(2022) Sheridan M. Hoy   DRUGS

Deuterated Drugs and Biomarkers in the COVID-19 Pandemic

(2022) Ross D. Jansen-van Vuuren et al.   ACS Omega

Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer

(2021) Yonggang Meng et al.   JOURNAL OF MEDICINAL CHEMISTRY

Combating TKI resistance in CML by inhibiting the PI3K/Akt/mTOR pathway in combination with TKIs: a review

(2021) Priyanka Singh et al.   MEDICAL ONCOLOGY

Properties of FDA-approved small molecule protein kinase inhibitors: a 2021 update

(2021) Robert Roskoski   PHARMACOLOGICAL RESEARCH

FGFR-TKI resistance in cancer: current status and perspectives

(2021) Sitong Yue et al.   Journal of Hematology & Oncology

Phase I clinical trial of HC ‐1119: A deuterated form of enzalutamide

(2021) Xiaoyu Li et al.   INTERNATIONAL JOURNAL OF CANCER

Donafenib Versus Sorafenib in First-Line Treatment of Unresectable or Metastatic Hepatocellular Carcinoma: A Randomized, Open-Label, Parallel-Controlled Phase II-III Trial

(2021) Shukui Qin et al.   JOURNAL OF CLINICAL ONCOLOGY

HER2-positive breast cancer and tyrosine kinase inhibitors: the time is now

(2021) Ilana Schlam et al.   npj Breast Cancer

Design and development of an oral remdesivir derivative VV116 against SARS-CoV-2

(2021) Yuanchao Xie et al.   CELL RESEARCH

Donafenib: First Approval

(2021) Susan J. Keam et al.   DRUGS

Small Molecule Kinase Inhibitor Drugs (1995–2021): Medical Indication, Pharmacology, and Synthesis

(2021) Cecilia C. Ayala-Aguilera et al.   JOURNAL OF MEDICINAL CHEMISTRY

Pharmacokinetics and brain distribution studies of 6-hydroxykynurenic acid and its structural modified compounds

(2021) Zhuowei Shen et al.   JOURNAL OF PHARMACY AND PHARMACOLOGY

Resistance to Tyrosine Kinase Inhibitors in Chronic Myeloid Leukemia—From Molecular Mechanisms to Clinical Relevance

(2021) Raquel Alves et al.   Cancers

Direct reversible decarboxylation from stable organic acids in dimethylformamide solution

(2020) Duanyang Kong et al.   SCIENCE

Limitations in Clinical Trials Leading to Anticancer Drug Approvals by the US Food and Drug Administration

(2020) Talal Hilal et al.   JAMA Internal Medicine

Electrolytic deuteration of unsaturated bonds without using D2

(2020) Aiko Kurimoto et al.   Nature Catalysis

Detailed molecular cytogenetic characterisation of the myeloid cell line U937 reveals the fate of homologous chromosomes and shows that centromere capture is a feature of genome instability

(2020) Ruth N. MacKinnon et al.   Molecular Cytogenetics

Applications of deuterium in medicinal chemistry

(2019) Tracey Pirali et al.   JOURNAL OF MEDICINAL CHEMISTRY

H–D Exchange Deuteration of Arenes at Room Temperature

(2019) Yoshinari Sawama et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Deuterated Curcuminoids: Synthesis, Structures, Computational/Docking and Comparative Cell Viability Assays against Colorectal Cancer

(2019) Kenneth K. Laali et al.   ChemMedChem

Design, synthesis of orally bioavailable novel anaplastic lymphoma kinase (ALK) inhibitor diphenylaminopyrimidine analogs and efficacy study on NCI-H2228 xenografts mice model

(2019) Debasis Das et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Molecular Mechanisms of Resistance to Tyrosine Kinase Inhibitors

(2019) Marjan Yaghmaie et al.   Current Hematologic Malignancy Reports

Thiazole-containing compounds as therapeutic targets for cancer therapy

(2019) Prabodh Chander Sharma et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design, synthesis and biological evaluation of deuterated Vismodegib for improving pharmacokinetic properties

(2018) Fangying Wang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Molecular targeted therapy: treating cancer with specificity

(2018) Yeuan Ting Lee et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Review of deutetrabenazine: a novel treatment for chorea associated with Huntington's disease

(2018) Marissa Dean et al.   Drug Design Development and Therapy

Drug metabolism in drug discovery and development

(2018) Zhoupeng Zhang et al.   Acta Pharmaceutica Sinica B

Role of Cytochrome P450 Enzymes in the Metabolic Activation of Tyrosine Kinase Inhibitors

(2018) Klarissa Jackson et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Deoxygenative Deuteration of Carboxylic Acids with D2 O

(2018) Muliang Zhang et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Evaluation of Deuterium-Labeled JNJ38877605: Pharmacokinetic, Metabolic, and in Vivo Antitumor Profiles

(2018) Zhengsheng Zhan et al.   CHEMICAL RESEARCH IN TOXICOLOGY

Deuterated drugs; updates and obviousness analysis

(2017) Graham S. Timmins   EXPERT OPINION ON THERAPEUTIC PATENTS

Biological and photochemical degradation of cytostatic drugs under laboratory conditions

(2017) Helena Franquet-Griell et al.   JOURNAL OF HAZARDOUS MATERIALS

Effect of N -methyl deuteration on pharmacokinetics and pharmacodynamics of enzalutamide

(2017) Xuehai Pang et al.   JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS

Current Challenges in Cancer Treatment

(2016) Jon Zugazagoitia et al.   CLINICAL THERAPEUTICS

Design, synthesis and biological evaluation of deuterated Tivozanib for improving pharmacokinetic properties

(2015) Shiwei Guo et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

A Simple and Cost-Effective Method for the Regioselective Deuteration of Phenols

(2015) Miao Zhan et al.   EUROPEAN JOURNAL OF ORGANIC CHEMISTRY

Design, synthesis and biological evaluation of deuterated nintedanib for improving pharmacokinetic properties

(2015) Ruixue Xu et al.   JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS

Key factors influencing ADME properties of therapeutic proteins: A need for ADME characterization in drug discovery and development

(2015) Jay Tibbitts et al.   mAbs

Ruthenium Catalyzed Selective α- and α,β-Deuteration of Alcohols Using D2O

(2015) Basujit Chatterjee et al.   ORGANIC LETTERS

Hodgkin Lymphoma Cell Lines Are Characterized by a Specific miRNA Expression Profile

(2015) Johan H. Gibcus et al.   NEOPLASIA

The kinetic deuterium isotope effect as applied to metabolic deactivation of imatinib to the des-methyl metabolite, CGP74588

(2013) Paul W. Manley et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Resistance to Tyrosine Kinase Inhibition Therapy for Chronic Myelogenous Leukemia: A Clinical Perspective and Emerging Treatment Options

(2013) Elias J. Jabbour et al.   Clinical Lymphoma Myeloma & Leukemia

The background, discovery and clinical development of BCR-ABL inhibitors

(2013) Gemma K. Lambert et al.   DRUG DISCOVERY TODAY

Using Deuterium in Drug Discovery: Leaving the Label in the Drug

(2013) Thomas G. Gant   JOURNAL OF MEDICINAL CHEMISTRY

PharmGKB summary

(2013) Daniella Lowenberg et al.   Pharmacogenetics and Genomics

Three new chondrosarcoma cell lines: one grade III conventional central chondrosarcoma and two dedifferentiated chondrosarcomas of bone

(2012) Jolieke G van Oosterwijk et al.   BMC CANCER

Understanding the mechanism of cytochrome P450 3A4: recent advances and remaining problems

(2012) Irina F. Sevrioukova et al.   DALTON TRANSACTIONS

A deuterated analog of dasatinib disrupts cell cycle progression and displays anti-non-small cell lung cancer activityin vitroandin vivo

(2012) Chunhua Ling et al.   INTERNATIONAL JOURNAL OF CANCER

Flavokawain B, a novel, naturally occurring chalcone, exhibits robust apoptotic effects and induces G2/M arrest of a uterine leiomyosarcoma cell line

(2012) Ramez N. Eskander et al.   JOURNAL OF OBSTETRICS AND GYNAECOLOGY RESEARCH

Ruthenium-Catalyzed Selective α,β-Deuteration of Bioactive Amines

(2012) Lorenz Neubert et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Mild Reaction Conditions for the Terminal Deuteration of Alkynes

(2012) Sean P. Bew et al.   ORGANIC LETTERS

Small-molecule protein kinase inhibitors and their effects on the immune system: implications for cancer treatment

(2011) Patrick A Ott et al.   Immunotherapy

Principles of early drug discovery

(2010) JP Hughes et al.   BRITISH JOURNAL OF PHARMACOLOGY

Characterization of stem cell attributes in human osteosarcoma cell lines

(2010) Lin Wang et al.   CANCER BIOLOGY & THERAPY

Synthesis of deuterium-labelled drugs by hydrogen-deuterium (H-D) exchange using heterogeneous catalysis

(2010) Nkaelang Modutlwa et al.   JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS

Lung Cancer Cell Lines as Tools for Biomedical Discovery and Research

(2010) Adi F. Gazdar et al.   JNCI-Journal of the National Cancer Institute

Cancer stem cells from colorectal cancer-derived cell lines

(2010) Trevor M. Yeung et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Breast Cancer Cell Lines Contain Functional Cancer Stem Cells with Metastatic Capacity and a Distinct Molecular Signature

(2009) Emmanuelle Charafe-Jauffret et al.   CANCER RESEARCH

Tyrosine Kinase Inhibitors – A Review on Pharmacology, Metabolism and Side Effects

(2009) Jorg Hartmann et al.   CURRENT DRUG METABOLISM

Identification and expansion of human osteosarcoma-cancer-stem cells by long-term 3-aminobenzamide treatment

(2009) Riccardo Di Fiore et al.   JOURNAL OF CELLULAR PHYSIOLOGY

CAL 27 is an oral adenosquamous carcinoma cell line

(2009) Lu Jiang et al.   ORAL ONCOLOGY

Molecular Profiling of Breast Cancer Cell Lines Defines Relevant Tumor Models and Provides a Resource for Cancer Gene Discovery

(2009) Jessica Kao et al.   PLoS One

A Convenient and Effective Method for the Regioselective Deuteration of Alcohols

(2008) Tomohiro Maegawa et al.   ADVANCED SYNTHESIS & CATALYSIS

A Simple, Cost-Effective Method for the Regioselective Deuteration of Anilines

(2008) Andrew Martins et al.   ORGANIC LETTERS

Efficient and Convenient Heterogeneous Palladium-Catalyzed Regioselective Deuteration at the Benzylic Position

(2007) Takanori Kurita et al.   CHEMISTRY-A EUROPEAN JOURNAL