Progress in the development of small molecular inhibitors of the Bruton’s tyrosine kinase (BTK) as a promising cancer therapy

Targeting therapy for prostate cancer by pharmaceutical and clinical pharmaceutical strategies

(2021) Wanxiao Sun et al.   JOURNAL OF CONTROLLED RELEASE

Transforming targeted cancer therapy with PROTACs: A forward-looking perspective

(2021) William Farnaby et al.   CURRENT OPINION IN PHARMACOLOGY

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

(2021) Xiao-Jing Pang et al.   MOLECULES

Clinical and biological implications of target occupancy in CLL treated with the BTK inhibitor acalabrutinib

(2020) Clare CHUI LING Sun et al.   BLOOD

Improvement of conventional anti-cancer drugs as new tools against multidrug resistant tumors

(2020) Sabrina Dallavalle et al.   DRUG RESISTANCE UPDATES

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

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

Efficient Targeted Degradation via Reversible and Irreversible Covalent PROTACs

(2020) Ronen Gabizon et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Discovery of quinoline-based irreversible BTK inhibitors

(2020) Gerjan de Bruin et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of potent and highly selective covalent inhibitors of Bruton’s tyrosine kinase bearing triazine scaffold

(2020) Yu Teng et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Characterization of a dual BET / HDAC inhibitor for treatment of pancreatic ductal adenocarcinoma

(2020) Xin Zhang et al.   INTERNATIONAL JOURNAL OF CANCER

Evaluating the Therapeutic Potential of Zanubrutinib in the Treatment of Relapsed/Refractory Mantle Cell Lymphoma: Evidence to Date

(2020) Yazeed Sawalha et al.   OncoTargets and Therapy

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

Progress in the Development of Small Molecular Inhibitors of Focal Adhesion Kinase (FAK)

(2020) Yang Lu et al.   JOURNAL OF MEDICINAL CHEMISTRY

HZ-A-005, a potent, selective, and covalent Bruton’s tyrosine kinase inhibitor in preclinical development

(2020) Wenhai Huang et al.   BIOORGANIC CHEMISTRY

Synthesis and biological activity of imidazole group-substituted arylaminopyrimidines (IAAPs) as potent BTK inhibitors against B-cell lymphoma and AML

(2020) Si Li et al.   BIOORGANIC CHEMISTRY

Proteolysis targeting chimera (PROTAC) in drug discovery paradigm: Recent progress and future challenges

(2020) Shenxin Zeng et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of novel chalcone-dithiocarbamates as ROS-mediated apoptosis inducers by inhibiting catalase

(2019) Dong-Jun Fu et al.   BIOORGANIC CHEMISTRY

Degradation of Bruton’s tyrosine kinase mutants by PROTACs for potential treatment of ibrutinib-resistant non-Hodgkin lymphomas

(2019) Yonghui Sun et al.   LEUKEMIA

PROTAC-Mediated Degradation of Bruton’s Tyrosine Kinase Is Inhibited by Covalent Binding

(2019) Christopher P. Tinworth et al.   ACS Chemical Biology

Mantle cell lymphoma: 2019 update on the diagnosis, pathogenesis, prognostication, and management

(2019) Preetesh Jain et al.   AMERICAN JOURNAL OF HEMATOLOGY

Discovery of pyrazolopyrimidine derivatives as potent BTK inhibitors with effective anticancer activity in MCL

(2019) Fansheng Ran et al.   BIOORGANIC CHEMISTRY

Genetic alterations and their clinical implications in DLBCL

(2019) Yi Miao et al.   Nature Reviews Clinical Oncology

Structural mechanism for Bruton’s tyrosine kinase activation at the cell membrane

(2019) Qi Wang et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Targeting BTK in CLL: Beyond Ibrutinib

(2019) David A. Bond et al.   Current Hematologic Malignancy Reports

Discovery and biological evaluation of N-(3-(7-((2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)amino)-4-methyl-2-oxo-2H-pyrimido[4,5-d][1,3]oxazin-1(4H)-yl)phenyl)acrylamide as potent Bruton’s tyrosine kinase inhibitors

(2019) Meng-zhen Lai et al.   ACTA PHARMACOLOGICA SINICA

Design, synthesis and biological evaluation of novel dithiocarbamate-substituted diphenylaminopyrimidine derivatives as BTK inhibitors

(2019) Zheng Zhai et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Some new anticancer platinum complexes of dithiocarbamate derivatives against human colorectal and pancreatic cell lines

(2019) Soudeh Hosseinzadeh et al.   JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS

Discovery and Biological evaluation of pyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione derivatives as potent Bruton’s tyrosine kinase inhibitors

(2019) Yanyan Diao et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Potency and Selectivity of BTK Inhibitors in Clinical Development for B-Cell Malignancies

(2019) Allard Kaptein et al.   Clinical Lymphoma Myeloma & Leukemia

Discovery and structure-activity relationship of novel diphenylthiazole derivatives as BTK inhibitor with potent activity against B cell lymphoma cell lines

(2019) Xiaofeng Guo et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Drug Discovery Targeting Anaplastic Lymphoma Kinase (ALK)

(2019) Xiaotian Kong et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton’s Tyrosine Kinase

(2019) Yunhang Guo et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Evobrutinib: An Oral, Potent, and Highly Selective, Covalent Bruton’s Tyrosine Kinase (BTK) Inhibitor for the Treatment of Immunological Diseases

(2019) Richard D. Caldwell et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design and synthesis of boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors

(2019) Jing Ren et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Discovery of 1,2,4-triazine-based derivatives as novel neddylation inhibitors and anticancer activity studies against gastric cancer MGC-803 cells

(2019) Jian Song et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Design and synthesis of novel 1-substituted 3-(6-phenoxypyridin-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine analogs as selective BTK inhibitors for the treatment of mantle cell lymphoma

(2019) Fansheng Ran et al.   BIOORGANIC CHEMISTRY

New 2,6,9-trisubstituted purine derivatives as Bcr-Abl and Btk inhibitors and as promising agents against leukemia

(2019) Jeanluc Bertrand et al.   BIOORGANIC CHEMISTRY

Combination of Gatekeeper Mutations and Cysteine 481 Replacement Causes Super Resistance to the Irreversible BTK Inhibitors Ibrutinib, Acalabrutinib and Zanubrutinib

(2019) Hernando Yesid Estupiñan Velasquez et al.   BLOOD

Final Results of Phase 1, Dose Escalation Study Evaluating ARQ 531 in Patients with Relapsed or Refractory B-Cell Lymphoid Malignancies

(2019) Jennifer Woyach et al.   BLOOD

Design, synthesis and biological evaluation of Proteolysis Targeting Chimeras (PROTACs) as a BTK degraders with improved pharmacokinetic properties

(2019) Saul Jaime-Figueroa et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Targeting the C481S Ibrutinib-Resistance Mutation in Bruton’s Tyrosine Kinase Using PROTAC-Mediated Degradation

(2018) Alexandru D. Buhimschi et al.   BIOCHEMISTRY

Design, synthesis and biological evaluation of novel 3-substituted pyrazolopyrimidine derivatives as potent Bruton’s tyrosine kinase (BTK) inhibitors

(2018) Nan Zheng et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Novel amino acid-substituted diphenylpyrimidine derivatives as potent BTK inhibitors against B cell lymphoma cell lines

(2018) Changyuan Wang et al.   BIOORGANIC & MEDICINAL CHEMISTRY

PROTAC-induced BTK degradation as a novel therapy for mutated BTK C481S induced ibrutinib-resistant B-cell malignancies

(2018) Yonghui Sun et al.   CELL RESEARCH

Discovery of novel 2,4-diarylaminopyrimidine analogues as ALK and ROS1 dual inhibitors to overcome crizotinib-resistant mutants including G1202R

(2018) Yu Wang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Identification of highly potent BTK and JAK3 dual inhibitors with improved activity for the treatment of B-cell lymphoma

(2018) Yang Ge et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Predicting the Conformational Variability of Abl Tyrosine Kinase using Molecular Dynamics Simulations and Markov State Models

(2018) Yilin Meng et al.   Journal of Chemical Theory and Computation

Role of Bruton’s tyrosine kinase in B cells and malignancies

(2018) Simar Pal Singh et al.   Molecular Cancer

Discovery and biological evaluation of N5-substituted 6,7-dioxo-6,7-dihydropteridine derivatives as potent Bruton's tyrosine kinase inhibitors

(2018) Haiyang Chen et al.   MedChemComm

Design and synthesis of benzofuro[3,2-b]pyridin-2(1H)-one derivatives as anti-leukemia agents by inhibiting Btk and PI3Kδ

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

Conversion of carbazole carboxamide based reversible inhibitors of Bruton’s tyrosine kinase (BTK) into potent, selective irreversible inhibitors in the carbazole, tetrahydrocarbazole, and a new 2,3-dimethylindole series

(2018) Qingjie Liu et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Identification of metabolites of evobrutinib in rat and human hepatocytes by using ultra-high performance liquid chromatography coupled with diode array detector and Q Exactive Orbitrap tandem mass spectrometry

(2018) Zeyun Li et al.   Drug Testing and Analysis

The BTK Inhibitor ARQ 531 Targets Ibrutinib-Resistant CLL and Richter Transformation

(2018) Sean D. Reiff et al.   Cancer Discovery

Bruton's Tyrosine Kinase degradation as a therapeutic strategy for cancer

(2018) Dennis Dobrovolsky et al.   BLOOD

Targeting Bruton’s Tyrosine Kinase Across B-Cell Malignancies

(2018) Caspar da Cunha-Bang et al.   DRUGS

Selective BTK inhibition improves bendamustine therapy response and normalizes immune effector functions in chronic lymphocytic leukemia

(2018) Eriong Lee-Vergés et al.   INTERNATIONAL JOURNAL OF CANCER

Discovery of 5,6-diaryl-1,2,4-triazines hybrids as potential apoptosis inducers

(2017) Dong-Jun Fu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design and synthesis of formononetin-dithiocarbamate hybrids that inhibit growth and migration of PC-3 cells via MAPK/Wnt signaling pathways

(2017) Dong-Jun Fu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Structural optimization of diphenylpyrimidine derivatives (DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B leukemia cell lines

(2017) Dan Zhao et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design and synthesis of sulfonamide-substituted diphenylpyrimidines (SFA-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B-cell lymphoblastic leukemia

(2017) He Liu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Bruton’s tyrosine kinase inhibitors: first and second generation agents for patients with Chronic Lymphocytic Leukemia (CLL)

(2017) Philip A Thompson et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Ability of Bruton’s Tyrosine Kinase Inhibitors to Sequester Y551 and Prevent Phosphorylation Determines Potency for Inhibition of Fc Receptor but not B-Cell Receptor Signaling

(2017) Andrew T. Bender et al.   MOLECULAR PHARMACOLOGY

Discovery of Potent and Selective Tricyclic Inhibitors of Bruton’s Tyrosine Kinase with Improved Druglike Properties

(2017) Xiaojing Wang et al.   ACS Medicinal Chemistry Letters

Bruton’s Tyrosine Kinase: An Emerging Key Player in Innate Immunity

(2017) Alexander N. R. Weber et al.   Frontiers in Immunology

Battling Btk Mutants With Noncovalent Inhibitors That Overcome Cys481 and Thr474 Mutations

(2016) Adam R. Johnson et al.   ACS Chemical Biology

Chronic lymphocytic leukemia (CLL)-Then and now

(2016) Kanti R. Rai et al.   AMERICAN JOURNAL OF HEMATOLOGY

Synthesis and biological evaluation of azole-diphenylpyrimidine derivatives (AzDPPYs) as potent T790M mutant form of epidermal growth factor receptor inhibitors

(2016) Zhendong Song et al.   BIOORGANIC & MEDICINAL CHEMISTRY

The Bruton Tyrosine Kinase (BTK) Inhibitor Acalabrutinib Demonstrates Potent On-Target Effects and Efficacy in Two Mouse Models of Chronic Lymphocytic Leukemia

(2016) Sarah E.M. Herman et al.   CLINICAL CANCER RESEARCH

Targeting Ibrutinib-Resistant BTK-C481S Mutation with ARQ 531, a Reversible Non-Covalent Inhibitor of BTK

(2016) Sudharshan Eathiraj et al.   Clinical Lymphoma Myeloma & Leukemia

Design strategies, structure activity relationship and mechanistic insights for purines as kinase inhibitors

(2016) Sahil Sharma et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Phase I study of single-agent CC-292, a highly selective Brutons tyrosine kinase inhibitor, in relapsed/refractory chronic lymphocytic leukemia

(2016) J. R. Brown et al.   HAEMATOLOGICA

Acalabrutinib (ACP-196): a selective second-generation BTK inhibitor

(2016) Jingjing Wu et al.   Journal of Hematology & Oncology

Second-generation inhibitors of Bruton tyrosine kinase

(2016) Jingjing Wu et al.   Journal of Hematology & Oncology

Bruton tyrosine kinase inhibitor ONO/GS-4059: from bench to bedside

(2016) Jingjing Wu et al.   Oncotarget

Phase I study of single-agent CC-292, a highly selective Brutons tyrosine kinase inhibitor, in relapsed/refractory chronic lymphocytic leukemia

(2016) J. R. Brown et al.   HAEMATOLOGICA

Abstract C186: SNS-062 is a potent noncovalent BTK inhibitor with comparable activity against wild type BTK and BTK with an acquired resistance mutation

(2015) Minke E. Binnerts et al.   MOLECULAR CANCER THERAPEUTICS

Discovery of a Potent, Covalent BTK Inhibitor for B-Cell Lymphoma

(2014) Hong Wu et al.   ACS Chemical Biology

Purine derivatives as potent Bruton’s tyrosine kinase (BTK) inhibitors for autoimmune diseases

(2014) Qing Shi et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Identification of novel PTP1B inhibitors by pharmacophore based virtual screening, scaffold hopping and docking

(2014) Vishal M. Balaramnavar et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Novel 2,4-Diarylaminopyrimidine Analogues (DAAPalogues) Showing Potent Inhibitory Activities against Both Wild-type and Mutant ALK Kinases

(2014) Zilan Song et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of a Series of 2,5-Diaminopyrimidine Covalent Irreversible Inhibitors of Bruton’s Tyrosine Kinase with in Vivo Antitumor Activity

(2014) Xitao Li et al.   JOURNAL OF MEDICINAL CHEMISTRY

Safety and activity of ibrutinib plus rituximab for patients with high-risk chronic lymphocytic leukaemia: a single-arm, phase 2 study

(2014) Jan A Burger et al.   LANCET ONCOLOGY

Ibrutinib and novel BTK inhibitors in clinical development

(2013) Akintunde Akinleye et al.   Journal of Hematology & Oncology

Fragment-Based Discovery of New Highly Substituted 1H-Pyrrolo[2,3-b]- and 3H-Imidazolo[4,5-b]-Pyridines as Focal Adhesion Kinase Inhibitors

(2013) Timo Heinrich et al.   JOURNAL OF MEDICINAL CHEMISTRY

1,3,5-Triazine as a Modular Scaffold for Covalent Inhibitors with Streamlined Target Identification

(2013) Ranjan Banerjee et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Discovery of a Mutant-Selective Covalent Inhibitor of EGFR that Overcomes T790M-Mediated Resistance in NSCLC

(2013) A. O. Walter et al.   Cancer Discovery

Design, synthesis and CoMFA studies of N1-amino acid substituted 2,4,5-triphenyl imidazoline derivatives as p53–MDM2 binding inhibitors

(2012) Chunqi Hu et al.   BIOORGANIC & MEDICINAL CHEMISTRY

BMX and Its Role in Inflammation, Cardiovascular Disease, and Cancer

(2012) Bruno Cenni et al.   INTERNATIONAL REVIEWS OF IMMUNOLOGY

The resurgence of covalent drugs

(2011) Juswinder Singh et al.   NATURE REVIEWS DRUG DISCOVERY

The Src, Syk, and Tec family kinases: Distinct types of molecular switches

(2010) J. Michael Bradshaw   CELLULAR SIGNALLING

Chronic active B-cell-receptor signalling in diffuse large B-cell lymphoma

(2010) R. Eric Davis et al.   NATURE

Identification ofN,1,4,4-Tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a Potent, Orally Available Cyclin Dependent Kinase Inhibitor

(2009) Maria Gabriella Brasca et al.   JOURNAL OF MEDICINAL CHEMISTRY

Novel mutant-selective EGFR kinase inhibitors against EGFR T790M

(2009) Wenjun Zhou et al.   NATURE

Novel N9-arenethenyl purines as potent dual Src/Abl tyrosine kinase inhibitors

(2008) Yihan Wang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

From Single- to Multi-Target Drugs in Cancer Therapy: When Aspecificity Becomes an Advantage

(2008) S. Giordano et al.   CURRENT MEDICINAL CHEMISTRY

Multiple Colorectal Neoplasms in X-Linked Agammaglobulinemia

(2007) Lodewijk A.A. Brosens et al.   Clinical Gastroenterology and Hepatology