Design, synthesis, and biological evaluation of nitroisoxazole-containing spiro[pyrrolidin-oxindole] derivatives as novel glutathione peroxidase 4/mouse double minute 2 dual inhibitors that inhibit breast adenocarcinoma cell proliferation

Discovery of novel akt1 inhibitor induces autophagy associated death in hepatocellular carcinoma cells

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

Fluorine-containing drugs approved by the FDA in 2019

(2020) Haibo Mei et al.   CHINESE CHEMICAL LETTERS

Novel HSP90-PI3K Dual Inhibitor Suppresses Melanoma Cell Proliferation by Interfering with HSP90-EGFR Interaction and Downstream Signaling Pathways

(2020) Qian Zhao et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Discovery of Thieno[2,3-d]pyrimidine-Based Hydroxamic Acid Derivatives as Bromodomain-Containing Protein 4/Histone Deacetylase Dual Inhibitors Induce Autophagic Cell Death in Colorectal Carcinoma Cells

(2020) Zhaoping Pan et al.   JOURNAL OF MEDICINAL CHEMISTRY

Selective covalent targeting of GPX4 using masked nitrile-oxide electrophiles

(2020) John K. Eaton et al.   Nature Chemical Biology

A Novel Redox Modulator Induces a GPX4-Mediated Cell Death That Is Dependent on Iron and Reactive Oxygen Species

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

Unconventional [2 + 3] Cyclization Involving [1,4]-Sulfonyl Transfer to Construct Polysubstituted Fluorazones as Inhibitors of Indoleamine 2,3-Dioxygenase 1

(2020) Xue Tang et al.   ORGANIC LETTERS

Structure–activity relationships of GPX4 inhibitor warheads

(2020) John K. Eaton et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Asymmetric synthesis of tetrahydroisoquinoline-fused spirooxindoles as Ras-GTP inhibitors that inhibit colon adenocarcinoma cell proliferation and invasion

(2018) Qian Zhao et al.   CHEMICAL COMMUNICATIONS

General Catalytic Enantioselective Access to Monohalomethyl and Trifluoromethyl Cyclopropanes

(2018) Wei-Sheng Huang et al.   CHEMISTRY-A EUROPEAN JOURNAL

Novel Allosteric Activators for Ferroptosis Regulator Glutathione Peroxidase 4

(2018) Cong Li et al.   JOURNAL OF MEDICINAL CHEMISTRY

p53 Suppresses Metabolic Stress-Induced Ferroptosis in Cancer Cells

(2018) Amy Tarangelo et al.   Cell Reports

Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents

(2018) Shipeng He et al.   JOURNAL OF MEDICINAL CHEMISTRY

A phase I study of SAR405838, a novel human double minute 2 (HDM2) antagonist, in patients with solid tumours

(2017) Maja de Jonge et al.   EUROPEAN JOURNAL OF CANCER

Discovery of 4-((3′R,4′S,5′R)-6″-Chloro-4′-(3-chloro-2-fluorophenyl)-1′-ethyl-2″-oxodispiro[cyclohexane-1,2′-pyrrolidine-3′,3″-indoline]-5′-carboxamido)bicyclo[2.2.2]octane-1-carboxylic Acid (AA-115/APG-115): A Potent and Orally Active Murine Double Minute 2 (MDM2) Inhibitor in Clinical Development

(2017) Angelo Aguilar et al.   JOURNAL OF MEDICINAL CHEMISTRY

Drug-tolerant persister cancer cells are vulnerable to GPX4 inhibition

(2017) Matthew J. Hangauer et al.   NATURE

Current Trends towards the Synthesis of Bioactive Heterocycles and Natural Products Using 1,3-Dipolar Cycloadditions (1,3-DC) with Azomethine Ylides

(2017) H. Döndas et al.   SYNTHESIS-STUTTGART

The Tumor Suppressor p53 Limits Ferroptosis by Blocking DPP4 Activity

(2017) Yangchun Xie et al.   Cell Reports

Trifluoromethyl nitrogen heterocycles: synthetic aspects and potential biological targets

(2016) F. Meyer   CHEMICAL COMMUNICATIONS

N-tert-Butylsulfinyl-3,3,3-trifluoroacetaldimine: Versatile Reagent for Asymmetric Synthesis of Trifluoromethyl-Containing Amines and Amino Acids of Pharmaceutical Importance

(2016) Haibo Mei et al.   EUROPEAN JOURNAL OF ORGANIC CHEMISTRY

Discovery of Novel Spiro[3H-indole-3,2′-pyrrolidin]-2(1H)-one Compounds as Chemically Stable and Orally Active Inhibitors of the MDM2–p53 Interaction

(2016) Andreas Gollner et al.   JOURNAL OF MEDICINAL CHEMISTRY

Targeting Programmed Cell Death Using Small-Molecule Compounds to Improve Potential Cancer Therapy

(2016) Bowen Ke et al.   MEDICINAL RESEARCH REVIEWS

Ferroptosis: Death by Lipid Peroxidation

(2016) Wan Seok Yang et al.   TRENDS IN CELL BIOLOGY

TP53 mutations emerge with HDM2 inhibitor SAR405838 treatment in de-differentiated liposarcoma

(2016) Joonil Jung et al.   Nature Communications

The asymmetric synthesis of CF3-containing spiro[pyrrolidin-3,2′-oxindole] through the organocatalytic 1,3-dipolar cycloaddition reaction

(2015) Mingxia Ma et al.   CHEMICAL COMMUNICATIONS

Recent Developments in the Trifluoromethylation of Alkynes

(2015) Pin Gao et al.   CHEMISTRY-A EUROPEAN JOURNAL

Recent Advances in the One-Step Synthesis of Distally Fluorinated Ketones

(2015) Yuwen Zeng et al.   CHEMISTRY-A EUROPEAN JOURNAL

SAR405838: A Novel and Potent Inhibitor of the MDM2:p53 Axis for the Treatment of Dedifferentiated Liposarcoma

(2015) K. L. J. Bill et al.   CLINICAL CANCER RESEARCH

Polyfluorinated groups in medicinal chemistry

(2015) Marcella Bassetto et al.   Future Medicinal Chemistry

6-(Trifluoromethyl)-2H-pyran-2-ones: Promising CF3-bearing conjugated cyclic diene and electrophilic building-blocks

(2015) Boris I. Usachev   JOURNAL OF FLUORINE CHEMISTRY

Ferroptosis as a p53-mediated activity during tumour suppression

(2015) Le Jiang et al.   NATURE

SAR405838: An Optimized Inhibitor of MDM2-p53 Interaction That Induces Complete and Durable Tumor Regression

(2014) S. Wang et al.   CANCER RESEARCH

Regulation of Ferroptotic Cancer Cell Death by GPX4

(2014) Wan Seok Yang et al.   CELL

Recent advances in the trifluoromethylation methodology and new CF3-containing drugs

(2014) Wei Zhu et al.   JOURNAL OF FLUORINE CHEMISTRY

Fluorine Modulates Species Selectivity in the Triazolopyrimidine Class of Plasmodium falciparum Dihydroorotate Dehydrogenase Inhibitors

(2014) Xiaoyi Deng et al.   JOURNAL OF MEDICINAL CHEMISTRY

Polypharmacology: Challenges and Opportunities in Drug Discovery

(2014) Andrew Anighoro et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery and saturation analysis of cancer genes across 21 tumour types

(2014) Michael S. Lawrence et al.   NATURE

Organocatalyzed asymmetric vinylogous Michael addition of α,β-unsaturated γ-butyrolactam

(2013) Jinlong Zhang et al.   CHEMICAL COMMUNICATIONS

Trifluoromethyl ketones: properties, preparation, and application

(2013) Christopher B. Kelly et al.   CHEMICAL COMMUNICATIONS

Mutational landscape and significance across 12 major cancer types

(2013) Cyriac Kandoth et al.   NATURE

Ferroptosis: An Iron-Dependent Form of Nonapoptotic Cell Death

(2012) Scott J. Dixon et al.   CELL

Multicomplex-Based Pharmacophore-Guided 3D-QSAR Studies of N-Substituted 2′-(Aminoaryl)Benzothiazoles as Aurora-A Inhibitors

(2012) Gu He et al.   Chemical Biology & Drug Design

Development of small-molecule probes that selectively kill cells induced to express mutant RAS

(2011) Michel Weïwer et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Catalysis for fluorination and trifluoromethylation

(2011) Takeru Furuya et al.   NATURE

Synthesis of Trifluoromethyl Pyrroles and Their Benzo Analogues

(2009) Günter Haufe et al.   SYNTHESIS-STUTTGART

The Many Roles for Fluorine in Medicinal Chemistry

(2008) William K. Hagmann   JOURNAL OF MEDICINAL CHEMISTRY