Impact of Cross-Coupling Reactions in Drug Discovery and Development

Discovery of potent epidermal growth factor receptor (EGFR) degraders by proteolysis targeting chimera (PROTAC)

(2020) Hao Zhang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

New Chemical Modalities and Strategic Thinking in Early Drug Discovery

(2020) Maria-Jesus Blanco et al.   ACS Medicinal Chemistry Letters

Recent Advances in Metal-Catalyzed Alkyl–Boron (C(sp3))–C(sp2)) Suzuki-Miyaura Cross-Couplings

(2020) Janwa El-Maiss et al.   Catalysts

Discovery of SHP2-D26 as a First, Potent, and Effective PROTAC Degrader of SHP2 Protein

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

Process Development Overcomes a Challenging Pd-Catalyzed C–N Coupling for the Synthesis of RORc Inhibitor GDC-0022

(2020) Lauren E. Sirois et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

A Facile Synthesis of Ligands for the von Hippel–Lindau E3 Ligase

(2020) Michael Gütschow et al.   SYNTHESIS-STUTTGART

Impact of Allosteric Modulation in Drug Discovery: Innovation in Emerging Chemical Modalities

(2020) Bingsong Han et al.   ACS Medicinal Chemistry Letters

PROTAC Technology: Opportunities and Challenges

(2020) Hongying Gao et al.   ACS Medicinal Chemistry Letters

Research and Development on Therapeutic Agents and Vaccines for COVID-19 and Related Human Coronavirus Diseases

(2020) Cynthia Liu et al.   ACS Central Science

Mild and Efficient Palladium-Mediated C–N Cross-Coupling Reaction between DNA-Conjugated Aryl Bromides and Aromatic Amines

(2019) Eduardo de Pedro Beato et al.   ACS Combinatorial Science

First targeted protein degrader hits the clinic

(2019) Asher Mullard   NATURE REVIEWS DRUG DISCOVERY

Allosteric Modalities for Membrane-Bound Receptors: Insights from Drug Hunting for Brain Diseases

(2019) Quinn Coughlin et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Buchwald-Hartwig Amination after 25 Years

(2019) Ruth Dorel et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Biphasic Aqueous Reaction Conditions for Process-Friendly Palladium-Catalyzed C–N Cross-Coupling of Aryl Amines

(2019) Subhash Pithani et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Targeting IRAK4 for Degradation with PROTACs

(2019) Joao Nunes et al.   ACS Medicinal Chemistry Letters

Cyclization of RGD Peptides by Suzuki–Miyaura Cross-Coupling

(2019) Isabell Kemker et al.   JOURNAL OF MEDICINAL CHEMISTRY

The future of cystic fibrosis care: a global perspective

(2019) Scott C Bell et al.   Lancet Respiratory Medicine

Mechanistic Development and Recent Applications of the Chan–Lam Amination

(2019) Matthew J. West et al.   CHEMICAL REVIEWS

Elexacaftor–Tezacaftor–Ivacaftor for Cystic Fibrosis with a Single Phe508del Allele

(2019) Peter G. Middleton et al.   NEW ENGLAND JOURNAL OF MEDICINE

Patent Review of Synthetic Routes and Crystalline Forms of the CFTR-Modulator Drugs Ivacaftor, Lumacaftor, Tezacaftor, and Elexacaftor

(2019) David L. Hughes   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Multikilogram Synthesis of a Potent Dual Bcl-2/Bcl-xL Antagonist. 1. Manufacture of the Acid Moiety and Development of Some Key Reactions

(2019) Christophe Hardouin et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Pd Metal Catalysts for Cross-Couplings and Related Reactions in the 21st Century: A Critical Review

(2018) Andrea Biffis et al.   CHEMICAL REVIEWS

Present drug-likeness filters in medicinal chemistry during the hit and lead optimization process: how far can they be simplified?

(2018) Serge Mignani et al.   DRUG DISCOVERY TODAY

Organic synthesis provides opportunities to transform drug discovery

(2018) David C. Blakemore et al.   Nature Chemistry

What Do You Get from DNA-Encoded Libraries?

(2018) Alexander L. Satz   ACS Medicinal Chemistry Letters

Discovery of AG-120 (Ivosidenib): A First-in-Class Mutant IDH1 Inhibitor for the Treatment of IDH1 Mutant Cancers

(2018) Janeta Popovici-Muller et al.   ACS Medicinal Chemistry Letters

Abemaciclib: a CDK4/6 inhibitor for the treatment of HR+/HER2– advanced breast cancer

(2018) Silvia Paola Corona et al.   Drug Design Development and Therapy

Evaluation of a non-prime site substituent and warheads combined with a decahydroisoquinolin scaffold as a SARS 3CL protease inhibitor

(2018) Kouji Ohnishi et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Application of Thiol-Modified Dual-Pore Silica Beads as a Practical Scavenger of Leached Palladium Catalyst in C–C Coupling Reactions

(2018) Tsuyoshi Yamada et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Lasmiditan for the treatment of migraine

(2017) Matilde Capi et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Discovery of Clinical Candidate 1-{[(2S,3S,4S)-3-Ethyl-4-fluoro-5-oxopyrrolidin-2-yl]methoxy}-7-methoxyisoquinoline-6-carboxamide (PF-06650833), a Potent, Selective Inhibitor of Interleukin-1 Receptor Associated Kinase 4 (IRAK4), by Fragment-Based Drug Design

(2017) Katherine L. Lee et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Necessary Nitrogen Atom: A Versatile High-Impact Design Element for Multiparameter Optimization

(2017) Lewis D. Pennington et al.   JOURNAL OF MEDICINAL CHEMISTRY

A Scale of Agonism and Allosteric Modulation for Assessment of Selectivity, Bias, and Receptor Mutation

(2017) Terry Kenakin   MOLECULAR PHARMACOLOGY

Tezacaftor–Ivacaftor in Patients with Cystic Fibrosis Homozygous for Phe508del

(2017) Jennifer L. Taylor-Cousar et al.   NEW ENGLAND JOURNAL OF MEDICINE

Asymmetric Suzuki-Miyaura coupling of heterocycles via Rhodium-catalysed allylic arylation of racemates

(2017) Philipp Schäfer et al.   Nature Communications

Evolving Green Chemistry Metrics into Predictive Tools for Decision Making and Benchmarking Analytics

(2017) Jun Li et al.   ACS Sustainable Chemistry & Engineering

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

(2017) Antoine Daina et al.   Scientific Reports

Discovery of substituted-2,4-dimethyl-(naphthalene-4-carbonyl)amino-benzoic acid as potent and selective EP4 antagonists

(2016) Maria-Jesus Blanco et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of potent aryl-substituted 3-[(3-methylpyridine-2-carbonyl) amino]-2,4-dimethyl-benzoic acid EP4 antagonists with improved pharmacokinetic profile

(2016) Maria-Jesus Blanco et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Identification and biological activity of 6-alkyl-substituted 3-methyl-pyridine-2-carbonyl amino dimethyl-benzoic acid EP4 antagonists

(2016) Maria-Jesus Blanco et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Applications of Palladium-Catalyzed C–N Cross-Coupling Reactions

(2016) Paula Ruiz-Castillo et al.   CHEMICAL REVIEWS

Largazole Analogues Embodying Radical Changes in the Depsipeptide Ring: Development of a More Selective and Highly Potent Analogue

(2016) Jehad Almaliti et al.   JOURNAL OF MEDICINAL CHEMISTRY

Chemical Space of DNA-Encoded Libraries

(2016) Raphael M. Franzini et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of 2-Indole-acylsulfonamide Myeloid Cell Leukemia 1 (Mcl-1) Inhibitors Using Fragment-Based Methods

(2016) Nicholas F. Pelz et al.   JOURNAL OF MEDICINAL CHEMISTRY

Industrial research: Drug companies must adopt green chemistry

(2016) John L. Tucker et al.   NATURE

Induced protein degradation: an emerging drug discovery paradigm

(2016) Ashton C. Lai et al.   NATURE REVIEWS DRUG DISCOVERY

DNA-encoded chemistry: enabling the deeper sampling of chemical space

(2016) Robert A. Goodnow et al.   NATURE REVIEWS DRUG DISCOVERY

Targeting BCL2 with Venetoclax in Relapsed Chronic Lymphocytic Leukemia

(2016) Andrew W. Roberts et al.   NEW ENGLAND JOURNAL OF MEDICINE

Stille coupling via C–N bond cleavage

(2016) Dong-Yu Wang et al.   Nature Communications

Recent Developments in Negishi Cross-Coupling Reactions

(2016) Diana Haas et al.   ACS Catalysis

Design and Synthesis of Biaryl DNA-Encoded Libraries

(2016) Yun Ding et al.   ACS Combinatorial Science

Stereospecific Nickel-Catalyzed Cross-Coupling Reactions of Benzylic Ethers and Esters

(2015) Emily J. Tollefson et al.   ACCOUNTS OF CHEMICAL RESEARCH

Discovery of selective N-[3-(1-methyl-piperidine-4-carbonyl)-phenyl]-benzamide-based 5-HT1F receptor agonists: Evolution from bicyclic to monocyclic cores

(2015) Deyi Zhang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Analysis of Past and Present Synthetic Methodologies on Medicinal Chemistry: Where Have All the New Reactions Gone?

(2015) Dean G. Brown et al.   JOURNAL OF MEDICINAL CHEMISTRY

A synthesis of abemaciclib utilizing a Leuckart–Wallach reaction

(2015) Michael O. Frederick et al.   TETRAHEDRON LETTERS

Escape from Flatland: Increasing Saturation as an Approach to Improving Clinical Success

(2009) Frank Lovering et al.   JOURNAL OF MEDICINAL CHEMISTRY