Molecular hybridization design and synthesis of novel spirooxindole-based MDM2 inhibitors endowed with BCL2 signaling attenuation; a step towards the next generation p53 activators

Structure-based design and optimization of pyrimidine- and 1,2,4-triazolo[4,3-a]pyrimidine-based matrix metalloproteinase-10/13 inhibitors via Dimroth rearrangement towards targeted polypharmacology

(2020) El Sayed Helmy El Ashry et al.   BIOORGANIC CHEMISTRY

Recent Small-Molecule Inhibitors of the p53–MDM2 Protein–Protein Interaction

(2020) Anastasia Beloglazkina et al.   MOLECULES

Synthesis, Anticancer Activity, and Molecular Modeling of New Halogenated Spiro[pyrrolidine-thiazolo-oxindoles] Derivatives

(2020) Mohammad Shahidul Islam et al.   Applied Sciences-Basel

Anticancer strategies by upregulating p53 through inhibition of its ubiquitination by MDM2

(2020) Abiodun Anifowose et al.   MEDICINAL CHEMISTRY RESEARCH

Unveiling the Reactivity of Cyclic Azomethine Ylides in [3+2] Cycloaddition Reactions within the Molecular Electron Density Theory

(2020) Luis R. Domingo et al.   EUROPEAN JOURNAL OF ORGANIC CHEMISTRY

Design and synthesis of new substituted spirooxindoles as potential inhibitors of the MDM2–p53 interaction

(2019) Assem Barakat et al.   BIOORGANIC CHEMISTRY

Design, synthesis and biological evaluation of novel α-acyloxy carboxamides via Passerini reaction as caspase 3/7 activators

(2019) Mohammed Salah Ayoup et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Dual VEGFR-2/PIM-1 kinase inhibition towards surmounting the resistance to antiangiogenic agents via hybrid pyridine and thienopyridine-based scaffolds: Design, synthesis and biological evaluation

(2019) Ola H. Rizk et al.   BIOORGANIC CHEMISTRY

Battle tactics against MMP-9; discovery of novel non-hydroxamate MMP-9 inhibitors endowed with PI3K/AKT signaling attenuation and caspase 3/7 activation via Ugi bis-amide synthesis

(2019) Mohammed Salah Ayoup et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Small-molecule Mcl-1 inhibitors: Emerging anti-tumor agents

(2018) Yichao Wan et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Global cancer statistics 2018: GLOBOCAN estimates of incidence and mortality worldwide for 36 cancers in 185 countries

(2018) Freddie Bray et al.   CA-A CANCER JOURNAL FOR CLINICIANS

Unravelling the Mysteries of [3+2] Cycloaddition Reactions

(2018) Mar Ríos-Gutiérez et al.   EUROPEAN JOURNAL OF ORGANIC CHEMISTRY

Synthesis of new thiazolo-pyrrolidine–(spirooxindole) tethered to 3-acylindole as anticancer agents

(2018) Mohammad Shahidul Islam et al.   BIOORGANIC CHEMISTRY

Resistance mechanisms to TP53-MDM2 inhibition identified by in vivo piggyBac transposon mutagenesis screen in an Arf−/−mouse model

(2017) Emilie A. Chapeau et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

p21: A Two-Faced Genome Guardian

(2017) Alexandros G. Georgakilas et al.   TRENDS IN MOLECULAR MEDICINE

Targeting the MDM2–p53 Protein–Protein Interaction for New Cancer Therapy: Progress and Challenges

(2017) Shaomeng Wang et al.   Cold Spring Harbor Perspectives in Medicine

SwissADME: a free web tool to evaluate pharmacokinetics, drug-likeness and medicinal chemistry friendliness of small molecules

(2017) Antoine Daina et al.   Scientific Reports

Apoptosis as anticancer mechanism: function and dysfunction of its modulators and targeted therapeutic strategies

(2016) Giuseppa Pistritto et al.   Aging-US

Spiro-oxindole derivative 5-chloro-4′,5′-diphenyl-3′-(4-(2-(piperidin-1-yl) ethoxy) benzoyl) spiro[indoline-3,2′-pyrrolidin]-2-one triggers apoptosis in breast cancer cells via restoration of p53 function

(2016) Ruchi Saxena et al.   INTERNATIONAL JOURNAL OF BIOCHEMISTRY & CELL BIOLOGY

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

Molecular Electron Density Theory: A Modern View of Reactivity in Organic Chemistry

(2016) Luis Domingo   MOLECULES

Maritoclax and dinaciclib inhibit MCL-1 activity and induce apoptosis in both a MCL-1-dependent and -independent manner

(2015) Shankar Varadarajan et al.   Oncotarget

Novel microscale approaches for easy, rapid determination of protein stability in academic and commercial settings

(2014) Crispin G. Alexander et al.   BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS

Maritoclax induces apoptosis in acute myeloid leukemia cells with elevated Mcl-1 expression

(2014) Kenichiro Doi et al.   CANCER BIOLOGY & THERAPY

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

(2014) S. Wang et al.   CANCER RESEARCH

Multiple p53-independent gene silencing mechanisms define the cellular response to p53 activation

(2014) Ramiro París et al.   CELL CYCLE

Design of Chemically Stable, Potent, and Efficacious MDM2 Inhibitors That Exploit the Retro-Mannich Ring-Opening-Cyclization Reaction Mechanism in Spiro-oxindoles

(2014) Angelo Aguilar et al.   JOURNAL OF MEDICINAL CHEMISTRY

MicroScale Thermophoresis: Interaction analysis and beyond

(2014) Moran Jerabek-Willemsen et al.   JOURNAL OF MOLECULAR STRUCTURE

Drugging the p53 pathway: understanding the route to clinical efficacy

(2014) Kian Hoe Khoo et al.   NATURE REVIEWS DRUG DISCOVERY

MDM2 Small-Molecule Antagonist RG7112 Activates p53 Signaling and Regresses Human Tumors in Preclinical Cancer Models

(2013) C. Tovar et al.   CANCER RESEARCH

Non-Cell-Autonomous Tumor Suppression by p53

(2013) Amaia Lujambio et al.   CELL

A threshold mechanism mediates p53 cell fate decision between growth arrest and apoptosis

(2013) M Kracikova et al.   CELL DEATH AND DIFFERENTIATION

Cancer Genome Landscapes

(2013) B. Vogelstein et al.   SCIENCE

Discovery of Potent and Orally Active p53-MDM2 Inhibitors RO5353 and RO2468 for Potential Clinical Development

(2013) Zhuming Zhang et al.   ACS Medicinal Chemistry Letters

Discovery of Marinopyrrole A (Maritoclax) as a Selective Mcl-1 Antagonist that Overcomes ABT-737 Resistance by Binding to and Targeting Mcl-1 for Proteasomal Degradation

(2012) Kenichiro Doi et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Microscale thermophoresis quantifies biomolecular interactions under previously challenging conditions

(2012) Susanne A.I. Seidel et al.   METHODS

Sunitinib induces apoptosis in pheochromocytoma tumor cells by inhibiting VEGFR2/Akt/mTOR/S6K1 pathways through modulation of Bcl-2 and BAD

(2011) Yuria Saito et al.   AMERICAN JOURNAL OF PHYSIOLOGY-ENDOCRINOLOGY AND METABOLISM

The Structure-Based Design of Mdm2/Mdmx-p53 Inhibitors Gets Serious

(2011) Grzegorz M. Popowicz et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Molecular Interaction Studies Using Microscale Thermophoresis

(2011) Moran Jerabek-Willemsen et al.   ASSAY AND DRUG DEVELOPMENT TECHNOLOGIES

Small-Molecule Inhibitors of p53-MDM2 Interaction: the 2006-2010 Update

(2011) Melissa Millard et al.   CURRENT PHARMACEUTICAL DESIGN

Apoptosis in cancer: from pathogenesis to treatment

(2011) Rebecca SY Wong   JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH

The p53-MDM2/MDMX axis – A chemotype perspective

(2011) Kareem Khoury et al.   MedChemComm

Understanding the High Reactivity of the Azomethine Ylides in [3 + 2] Cycloaddition Reactions

(2010) Luis R. Domingo et al.   LETTERS IN ORGANIC CHEMISTRY

Protein-binding assays in biological liquids using microscale thermophoresis

(2010) Christoph J. Wienken et al.   Nature Communications

Inhibitors of MDM2 and MDMX: a structural perspective

(2009) Christiane Riedinger et al.   Future Medicinal Chemistry

The genetics of the p53 pathway, apoptosis and cancer therapy

(2008) Alexei Vazquez et al.   NATURE REVIEWS DRUG DISCOVERY