FDA-approved pyrimidine-fused bicyclic heterocycles for cancer therapy: synthesis and clinical application

Synthetic Approaches to New Drugs Approved during 2018

(2020) Andrew C. Flick et al.   JOURNAL OF MEDICINAL CHEMISTRY

Tucatinib: First Approval

(2020) Arnold Lee   DRUGS

New Drug Approvals for 2019: Synthesis and Clinical Applications

(2020) Shuo Yuan et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Drug repurposing: Discovery of troxipide analogs as potent antitumor agents

(2020) Nan Lu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of tofacitinib derivatives as orally active antitumor agents based on the scaffold hybridization strategy

(2020) Xiao-Jing Shi et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of new [1,2,4] Triazolo[1,5-a]Pyrimidine derivatives that Kill gastric cancer cells via the mitochondria pathway

(2020) Shuai Wang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Structure-Based Design, Synthesis, and Biological Evaluation of New Triazolo[1,5-a]Pyrimidine Derivatives as Highly Potent and Orally Active ABCB1 Modulators

(2020) Shuai Wang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of [1,2,4]triazolo[1,5-a]pyrimidines derivatives as potential anticancer agents

(2020) Jin-Ling Huo et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Larotrectinib: First Global Approval

(2019) Lesley J. Scott   DRUGS

Development of the triazole-fused pyrimidine derivatives as highly potent and reversible inhibitors of histone lysine specific demethylase 1 (LSD1/KDM1A)

(2019) Zhonghua Li et al.   Acta Pharmaceutica Sinica B

Development of Highly Potent, Selective, and Cellular Active Triazolo[1,5-a]pyrimidine-Based Inhibitors Targeting the DCN1–UBC12 Protein–Protein Interaction

(2019) Shuai Wang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Designing influenza polymerase acidic endonuclease inhibitors via ‘privileged scaffold’ re-evolution/refining strategy

(2019) Han Ju et al.   Future Medicinal Chemistry

Experience-based discovery (EBD) of aryl hydrazines as new scaffolds for the development of LSD1/KDM1A inhibitors

(2019) Zhong-Rui Li et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis, structure-activity relationship studies and biological characterization of new [1,2,4]triazolo[1,5-a]pyrimidine-based LSD1/KDM1A inhibitors

(2019) Shuai Wang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthetic Approaches to the New Drugs Approved During 2017

(2019) Andrew C. Flick et al.   JOURNAL OF MEDICINAL CHEMISTRY

Quinolone derivatives: Potential anti‐HIV agent—development and application

(2019) Ruo Wang et al.   ARCHIV DER PHARMAZIE

Perspectives of medicinally privileged chalcone based metal coordination compounds for biomedical applications

(2019) Debarshi Kar Mahapatra et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of WS-157 as a highly potent, selective and orally active EGFR inhibitor

(2019) Pengxing He et al.   Acta Pharmaceutica Sinica B

Medicinal chemistry of indole derivatives: Current to future therapeutic prospectives

(2019) Archana Kumari et al.   BIOORGANIC CHEMISTRY

Heterocycles in Medicinal Chemistry

(2019) Josef Jampilek   MOLECULES

Targeting autophagy-related protein kinases for potential therapeutic purpose

(2019) Honggang Xiang et al.   Acta Pharmaceutica Sinica B

Discovery of [1,2,3]triazolo[4,5-d]pyrimidine derivatives as highly potent, selective, and cellularly active USP28 inhibitors

(2019) Zhenzhen Liu et al.   Acta Pharmaceutica Sinica B

Synthetic Approaches to New Drugs Approved During 2016

(2018) Andrew C. Flick et al.   JOURNAL OF MEDICINAL CHEMISTRY

Pembrolizumab plus Chemotherapy in Metastatic Non–Small-Cell Lung Cancer

(2018) Leena Gandhi et al.   NEW ENGLAND JOURNAL OF MEDICINE

6-Thioguanine is a noncompetitive and slow binding inhibitor of human deubiquitinating protease USP2

(2018) Shang-Ju Chuang et al.   Scientific Reports

Discovery of a non-toxic [1,2,4]triazolo[1,5-a]pyrimidin-7-one (WS-10) that modulates ABCB1-mediated multidrug resistance (MDR)

(2018) Liming Chang et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Dacomitinib: First Global Approval

(2018) Matt Shirley   DRUGS

Duvelisib: First Global Approval

(2018) Hannah A. Blair   DRUGS

Design, synthesis and biological evaluation of [1,2,4]triazolo[1,5-a]pyrimidines as potent lysine specific demethylase 1 (LSD1/KDM1A) inhibitors

(2017) Shuai Wang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthetic Approaches to the New Drugs Approved During 2015

(2017) Andrew C. Flick et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthetic approaches to the 2014 new drugs

(2016) Andrew C. Flick et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Inverse agonism at the P2Y12 receptor and ENT1 transporter blockade contribute to platelet inhibition by ticagrelor

(2016) R. Aungraheeta et al.   BLOOD

Olmutinib: First Global Approval

(2016) Esther S. Kim   DRUGS

The safety of vandetanib for the treatment of thyroid cancer

(2016) Venessa H. M. Tsang et al.   Expert Opinion On Drug Safety

Raltitrexed Inhibits HepG2 Cell Proliferation via G0/G1 Cell Cycle Arrest

(2016) Hongwei Zhao et al.   ONCOLOGY RESEARCH

Targeting PI3Kδ and PI3Kγ signalling disrupts human AML survival and bone marrow stromal cell mediated protection

(2016) Genevra Pillinger et al.   Oncotarget

EGFR Exon 18 Mutations in Lung Cancer: Molecular Predictors of Augmented Sensitivity to Afatinib or Neratinib as Compared with First- or Third-Generation TKIs

(2015) Y. Kobayashi et al.   CLINICAL CANCER RESEARCH

Molecular Pathways: Targeting the Cyclin D-CDK4/6 Axis for Cancer Treatment

(2015) T. VanArsdale et al.   CLINICAL CANCER RESEARCH

FDA Approval: Palbociclib for the Treatment of Postmenopausal Patients with Estrogen Receptor-Positive, HER2-Negative Metastatic Breast Cancer

(2015) J. A. Beaver et al.   CLINICAL CANCER RESEARCH

Heterocyclic Scaffolds: Centrality in Anticancer Drug Development

(2015) Imran Ali et al.   CURRENT DRUG TARGETS

Afatinib versus cisplatin-based chemotherapy for EGFR mutation-positive lung adenocarcinoma (LUX-Lung 3 and LUX-Lung 6): analysis of overall survival data from two randomised, phase 3 trials

(2015) James Chih-Hsin Yang et al.   LANCET ONCOLOGY

Direct and two-step bioorthogonal probes for Bruton's tyrosine kinase based on ibrutinib: a comparative study

(2015) Nora Liu et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

An Oncogenic NTRK Fusion in a Patient with Soft-Tissue Sarcoma with Response to the Tropomyosin-Related Kinase Inhibitor LOXO-101

(2015) R. C. Doebele et al.   Cancer Discovery

“Old Friends in New Guise”: Exploiting Privileged Structures for Scaffold Re-Evolution/Refining

(2014) Yu'ning Song et al.   COMBINATORIAL CHEMISTRY & HIGH THROUGHPUT SCREENING

Ibrutinib: a first in class covalent inhibitor of Bruton's tyrosine kinase

(2014) Matthew S Davids et al.   Future Oncology

Raltitrexed induces mitochondrial-mediated apoptosis in SGC7901 human gastric cancer cells

(2014) SONG XUE et al.   Molecular Medicine Reports

Comparison of the Efficacy and Safety of EFGR Tyrosine Kinase Inhibitor Monotherapy with Standard Second-line Chemotherapy in Previously Treated Advanced Non-small-cell Lung Cancer: a Systematic Review and Meta-analysis

(2013) Wei-Xiang Qi et al.   Asian Pacific Journal of Cancer Prevention

Design, synthesis and biological evaluation of novel 4-anilinoquinazolines with C-6 urea-linked side chains as inhibitors of the epidermal growth factor receptor

(2013) Xu Zhang et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Dual CDK4/CDK6 Inhibition Induces Cell-Cycle Arrest and Senescence in Neuroblastoma

(2013) J. Rader et al.   CLINICAL CANCER RESEARCH

Heterocycle-thioacetic Acid Motif: A Privileged Molecular Scaffold with Potent, Broad-Ranging Pharmacological Activities

(2013) Yu’ning Song et al.   CURRENT PHARMACEUTICAL DESIGN

Afatinib: First Global Approval

(2013) Rosselle T. Dungo et al.   DRUGS

Novel heterocyclic-fused pyrimidine derivatives: Synthesis, molecular modeling and pharmacological screening

(2013) Reem K. Arafa et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Palbociclib (PD 0332991): targeting the cell cycle machinery in breast cancer

(2013) Andrea Rocca et al.   EXPERT OPINION ON PHARMACOTHERAPY

The Selectivity and Potency of the New PDE5 Inhibitor TPN729MA

(2013) Zhen Wang et al.   Journal of Sexual Medicine

A Stereoselective Process for the Manufacture of a 2′-Deoxy-β-d-Ribonucleoside Using the Vorbrüggen Glycosylation

(2013) Julian P. Henschke et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Inhibitors of BTK and ITK: State of the New Drugs for Cancer, Autoimmunity and Inflammatory Diseases

(2013) L. Vargas et al.   SCANDINAVIAN JOURNAL OF IMMUNOLOGY

Epidermal growth factor receptor (EGFR) mutation and personalized therapy in advanced nonsmall cell lung cancer (NSCLC)

(2013) Kunihiko Kobayashi et al.   Targeted Oncology

Vandetanib, an Inhibitor of VEGF Receptor-2 and EGF Receptor, Suppresses Tumor Development and Improves Prognosis of Liver Cancer in Mice

(2012) K. Inoue et al.   CLINICAL CANCER RESEARCH

The role of clofarabine in acute myeloid leukemia

(2012) Hady Ghanem et al.   LEUKEMIA & LYMPHOMA

Bruton tyrosine kinase represents a promising therapeutic target for treatment of chronic lymphocytic leukemia and is effectively targeted by PCI-32765

(2011) S. E. M. Herman et al.   BLOOD

Therapeutic potential of cladribine in combination with STAT3 inhibitor against multiple myeloma

(2011) Jian Ma et al.   BMC CANCER

A New Synthesis of 2-chloro-2′-deoxyadenosine (Cladribine), CdA)

(2011) Shaohong Xu et al.   NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS

The Bruton tyrosine kinase inhibitor PCI-32765 ameliorates autoimmune arthritis by inhibition of multiple effector cells

(2011) Betty Y Chang et al.   ARTHRITIS RESEARCH & THERAPY

CAL-101, a p110  selective phosphatidylinositol-3-kinase inhibitor for the treatment of B-cell malignancies, inhibits PI3K signaling and cellular viability

(2010) B. J. Lannutti et al.   BLOOD

Phosphatidylinositol 3-kinase-  inhibitor CAL-101 shows promising preclinical activity in chronic lymphocytic leukemia by antagonizing intrinsic and extrinsic cellular survival signals

(2010) S. E. M. Herman et al.   BLOOD

Pralatrexate Is Synergistic with the Proteasome Inhibitor Bortezomib in In vitro and In vivo Models of T-Cell Lymphoid Malignancies

(2010) E. Marchi et al.   CLINICAL CANCER RESEARCH

Selective Inhibition of JAK1 and JAK2 Is Efficacious in Rodent Models of Arthritis: Preclinical Characterization of INCB028050

(2010) J. S. Fridman et al.   JOURNAL OF IMMUNOLOGY

Administration of a Tropomyosin Receptor Kinase Inhibitor Attenuates Sarcoma-Induced Nerve Sprouting, Neuroma Formation and Bone Cancer Pain

(2010) Joseph R Ghilardi et al.   Molecular Pain

A Placebo-Controlled Trial of Oral Cladribine for Relapsing Multiple Sclerosis

(2010) Gavin Giovannoni et al.   NEW ENGLAND JOURNAL OF MEDICINE

Efficient Syntheses of Clofarabine and Gemcitabine From 2-Deoxyribonolactone

(2010) Yana Cen et al.   NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS

In Vitro and Ex Vivo Testing of Tenofovir Shows It Is Effective As an HIV-1 Microbicide

(2010) Lisa C. Rohan et al.   PLoS One

The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy

(2010) L. A. Honigberg et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Mechanisms of anti-cancer action and pharmacology of clofarabine

(2009) Anna Zhenchuk et al.   BIOCHEMICAL PHARMACOLOGY

6-Thioguanine Perturbs Cytosine Methylation at the CpG Dinucleotide Site by DNA Methyltransferasesin Vitroand Acts as a DNA Demethylating Agentin Vivo†

(2009) Hongxia Wang et al.   BIOCHEMISTRY

Discovery of A Novel Her-1/Her-2 Dual Tyrosine Kinase Inhibitor for the Treatment of Her-1 Selective Inhibitor-Resistant Non-small Cell Lung Cancer

(2009) Mi Young Cha et al.   JOURNAL OF MEDICINAL CHEMISTRY

Pemetrexed in the treatment of advanced non-squamous lung cancer

(2009) Antonio Rossi et al.   LUNG CANCER

Approval Summary: Pemetrexed in the Initial Treatment of Advanced/Metastatic Non-Small Cell Lung Cancer

(2009) M. H. Cohen et al.   ONCOLOGIST

A novel approach to quinazolin-4(3H)-one via quinazoline oxidation: an improved synthesis of 4-anilinoquinazolines

(2009) Giovanni Marzaro et al.   TETRAHEDRON

Lapatinib: A dual inhibitor of human epidermal growth factor receptor tyrosine kinases

(2008) P MEDINA et al.   CLINICAL THERAPEUTICS

Apoptosis-inducing effect of erlotinib is potentiated by 3,3′-diindolylmethane in vitro and in vivo using an orthotopic model of pancreatic cancer

(2008) Shadan Ali et al.   MOLECULAR CANCER THERAPEUTICS

BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models

(2008) D Li et al.   ONCOGENE

FDA Drug Approval Summary: Nelarabine (Arranon(R)) for the Treatment of T-Cell Lymphoblastic Leukemia/Lymphoma

(2008) M. H. Cohen et al.   ONCOLOGIST