4.4 Article

Discovery of pyrazolopyrimidines that selectively inhibit CSF-1R kinase by iterative design, synthesis and screening against glioblastoma cells

Related references

Note: Only part of the references are listed.
Review Chemistry, Medicinal

CSF1R inhibitors are emerging immunotherapeutic drugs for cancer treatment

Jiachen Wen et al.

Summary: Colony-Stimulating Factor-1 Receptor (CSF1R) is a receptor tyrosine kinase that plays a crucial role in the differentiation and maintenance of macrophages and osteoclasts. Inhibiting CSF1R activity has emerged as a promising strategy for cancer treatment and may have potential applications in other fields.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2023)

Review Chemistry, Medicinal

Pyrazolo[3,4-d]pyrimidine scaffold: A review on synthetic approaches and EGFR and VEGFR inhibitory activities

Asmaa E. Kassab

Summary: The pyrazolo[3,4-d]pyrimidine core is a promising framework for drug design and discovery, mimicking kinase active site hinge region binding contacts. It has a wide range of pharmacological and biological value, particularly as an anticancer agent. This review summarizes the main synthetic routes of pyrazolo[3,4-d]pyrimidines and their recent developments as inhibitors of endothelial growth factor receptors and vascular endothelial growth factor receptors, aiming to guide the design and synthesis of novel pyrazolo[3,4-d]pyrimidine derivatives for clinical use in cancer treatment.

ARCHIV DER PHARMAZIE (2023)

Article Chemistry, Medicinal

DruMAP: A Novel Drug Metabolism and Pharmacokinetics Analysis Platform

Hitoshi Kawashima et al.

Summary: We have developed a novel drug metabolism and pharmacokinetics (DMPK) analysis platform called DruMAP. It includes a database for DMPK parameters and programs that can predict multiple DMPK parameters based on the chemical structure of a compound. The database contains curated DMPK parameters from public sources, in-house experimental data, and predicted DMPK parameters from our programs. Users can simultaneously predict several DMPK parameters for novel compounds not found in the database. The platform provides a simple tool for searching and predicting DMPK parameters, contributing to the acceleration of new drug development.

JOURNAL OF MEDICINAL CHEMISTRY (2023)

Article Chemistry, Medicinal

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

Cecilia C. Ayala-Aguilera et al.

Summary: Kinase inhibitors play a central role in the treatment of progressive disorders, with FDA approving 73 small molecule kinase inhibitor drugs by September 2021. This review summarizes the therapeutic and pharmacological properties of approved kinase inhibitors, as well as their synthesis routes, with an update on drugs approved in 2021.

JOURNAL OF MEDICINAL CHEMISTRY (2022)

Article Biotechnology & Applied Microbiology

Phenotypic drug discovery: recent successes, lessons learned and new directions

Fabien Vincent et al.

Summary: Phenotypic drug discovery has re-emerged as a systematic approach to drug discovery based on therapeutic effects in realistic disease models. This article discusses recent successes with this approach and explores ongoing challenges and strategies to address them.

NATURE REVIEWS DRUG DISCOVERY (2022)

Review Chemistry, Multidisciplinary

Targeting tumor cells with pyrazolo[3,4-d] pyrimidine scaffold: A literature review on synthetic approaches, structure activity relationship, structural and target-based mechanisms

Mohamed A. Abdelgawad et al.

Summary: This review discusses the antitumor potential, mechanisms of action, and structure-activity relationship studies of Pyrazolo[3,4-d]pyrimidine compounds. By optimizing this ring system, it is expected to discover new drugs with better selectivity and increased anticancer potential.

ARABIAN JOURNAL OF CHEMISTRY (2022)

Article Biotechnology & Applied Microbiology

Improving target assessment in biomedical research: the GOT-IT recommendations

Christoph H. Emmerich et al.

Summary: Academic research plays a crucial role in identifying new drug targets, and this Perspective introduces a framework to assist academic scientists and funders in prioritizing target assessment activities to achieve scientific goals and objectives related to licensing, industry collaboration, and clinical trials.

NATURE REVIEWS DRUG DISCOVERY (2021)

Review Oncology

A Review of Newly Diagnosed Glioblastoma

Bryan Oronsky et al.

Summary: Glioblastoma is an aggressive primary intra-axial brain tumor with poor prognosis, and current treatment involves surgery, radiotherapy, and chemotherapy. This review summarizes the characteristics, current treatment options, and potential future therapeutic prospects for the disease.

FRONTIERS IN ONCOLOGY (2021)

Article Oncology

A Conformation Selective Mode of Inhibiting SRC Improves Drug Efficacy and Tolerability

Carolin Temps et al.

Summary: The study highlights the potential of a small molecule, eCF506, to inhibit both catalytic and scaffolding functions of SRC, leading to increased anticancer properties and tolerability compared to other SRC/ABL inhibitors.

CANCER RESEARCH (2021)

Review Pharmacology & Pharmacy

Glioblastoma multiforme (GBM): An overview of current therapies and mechanisms of resistance

Wei Wu et al.

Summary: Glioblastoma multiforme (GBM) is the most common malignant primary brain tumor with highly infiltrative nature and treatment resistance, highlighting the importance of innovative treatment strategies. The standard treatment for GBM is surgical resection followed by chemoradiotherapy, but the robust DNA repair and self-renewing capabilities of GBM cells lead to resistance against current therapies.

PHARMACOLOGICAL RESEARCH (2021)

Article Biochemistry & Molecular Biology

Pyrazolopyrimide library screening in glioma cells discovers highly potent antiproliferative leads that target the PI3K/mTOR pathway

Teresa Valero et al.

BIOORGANIC & MEDICINAL CHEMISTRY (2020)

Review Immunology

To Kill a Microglia: A Case for CSF1R Inhibitors

Kim N. Green et al.

TRENDS IN IMMUNOLOGY (2020)

Article Cell Biology

CSF1R signaling is a regulator of pathogenesis in progressive MS

Nellwyn Hagan et al.

CELL DEATH & DISEASE (2020)

Review Biochemistry & Molecular Biology

Recent developments in anticancer kinase inhibitors based on the pyrazolo[3,4-d]pyrimidine scaffold

Daniel J. Baillache et al.

RSC MEDICINAL CHEMISTRY (2020)

Article Chemistry, Medicinal

Recent Advances of Colony-Stimulating Factor-1 Receptor (CSF-1R) Kinase and Its Inhibitors

Mohammed El-Gamal et al.

JOURNAL OF MEDICINAL CHEMISTRY (2018)

Article Chemistry, Multidisciplinary

Bioorthogonal Uncaging of the Active Metabolite of Irinotecan by Palladium-Functionalized Microdevices

Catherine Adam et al.

CHEMISTRY-A EUROPEAN JOURNAL (2018)

Article Chemistry, Medicinal

Lowering Lipophilicity by Adding Carbon: One-Carbon Bridges of Morpholines and Piperazines

Sebastien L. Degorce et al.

JOURNAL OF MEDICINAL CHEMISTRY (2018)

Article Biochemistry & Molecular Biology

Coral: Clear and Customizable Visualization of Human Kinome Data

Kathleen S. Metz et al.

CELL SYSTEMS (2018)

Article Chemistry, Medicinal

Synthesis and structure-activity relationship study of pyrazolo[3,4-d]pyrimidines as tyrosine kinase RET inhibitors

Chengyan Wang et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2017)

Article Chemistry, Medicinal

Discovery of pyrazolopyrimidine derivatives as novel inhibitors of ataxia telangiectasia and rad3 related protein (ATR)

Sreekanth A. Ramachandran et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2017)

Review Chemistry, Medicinal

Next-generation phenotypic screening

Scott J. Warchal et al.

FUTURE MEDICINAL CHEMISTRY (2016)

Article Chemistry, Medicinal

Small Molecule Kinase Inhibitors for the Treatment of Brain Cancer

Timothy P. Heffron

JOURNAL OF MEDICINAL CHEMISTRY (2016)

Article Biochemical Research Methods

Cell Painting, a high-content image-based assay for morphological profiling using multiplexed fluorescent dyes

Mark-Anthony Bray et al.

NATURE PROTOCOLS (2016)

Article Cell Biology

Origin of the U87MG glioma cell line: Good news and bad news

Marie Allen et al.

SCIENCE TRANSLATIONAL MEDICINE (2016)

Article Biochemistry & Molecular Biology

eCF309: a potent, selective and cell-permeable mTOR inhibitor

Craig Fraser et al.

MEDCHEMCOMM (2016)

Article Chemistry, Medicinal

UNC2025, a Potent and Orally Bioavailable MER/FLT3 Dual Inhibitor

Weihe Zhang et al.

JOURNAL OF MEDICINAL CHEMISTRY (2014)

Review Oncology

Macrophage colony-stimulating factor and cancer: a review

S. Chockalingam et al.

TUMOR BIOLOGY (2014)

Editorial Material Pharmacology & Pharmacy

Phenotypic vs. Target-Based Drug Discovery for First-in-Class Medicines

D. C. Swinney

CLINICAL PHARMACOLOGY & THERAPEUTICS (2013)

Review Pharmacology & Pharmacy

Phenotypic screens as a renewed approach for drug discovery

Wei Zheng et al.

DRUG DISCOVERY TODAY (2013)

Article Chemistry, Medicinal

UNC1062, a new and potent Mer inhibitor

Jing Liu et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2013)

Article Multidisciplinary Sciences

Multiplex Cytological Profiling Assay to Measure Diverse Cellular States

Sigrun M. Gustafsdottir et al.

PLOS ONE (2013)

Article Chemistry, Medicinal

Preparation of 3-Substituted-1-Isopropyl-1H-pyrazolo[3,4-d]pyrimidin-4-amines as RET Kinase Inhibitors

Peter Diner et al.

JOURNAL OF MEDICINAL CHEMISTRY (2012)

Article Biochemistry & Molecular Biology

Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases

Beth Apsel et al.

NATURE CHEMICAL BIOLOGY (2008)