Synfacts

Category: Chemistry in Medicine and Biology

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Issue 08/2022

Synthesis and Biological Evaluation of Alkaloid GB18
Expanding Horizons: Piperazinobenzodiazepinones as Alphavirus Inhibitors
Targeted Chemotherapy Using in Vivo Transition Metal Catalysis
Is Further Rhodamine Functionalization Beneficial? Si
Synthesis of Bioactive Euphane Triterpenoid System
Extracting Unique Structures from Nature: A Potential anti-Covid Agent Synthesis
Synthesis of MK-2305 via Enantioselective Hydrogenation of a Tetrasubstituted Olefin
A Potent Allosteric Inhibitor of HIV-1 Integrase
Optimized Oxazocine Inhibitor of Mutant KRASG12C
Fluorescent BODIPY Caged by Azobenzene
The Hidden Symmetry of (±)-Histrionicotoxin
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Issue 07/2022

A Natural Product Hybrid with Potent Antitumor Activity
Breaking the Mirror: Deracemization of α-Branched Aldehydes
Harnessing the Power of Organo- and Biocatalysis to Synthesize STING Agonist MK-1454
Unexpected Hydrolytic Triazoloquinazoline Ring Opening Leads to a Potent HDAC6 Inhibitor
Expanding the E3 Ligase Toolbox by Co-opting Methyl Readers
Novel Macrocycle-Based Type-II TRK Inhibitors
A Rapid Approach to Cyclopropane-Fused Lactams
Tuning Colors of the Drug: A Systematic Study of the Emissive Features of the Deferasirox Scaffold
A Reversible Covalent Inhibitor Targeting the BCR-ABL Active-Site Lysine
Fluorogenic Cyclopropenones for Cellular Imaging
An Improved Orthosteric Antagonist of the M5 Muscarinic Acetylcholine Receptor
A Diastereoselective Cyclopropanation Strategy
The First Total Synthesis of Bryostatin 7
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Issue 06/2022

Targeted Protein Stabilization with DUBTACs
Take it Easy on the Synthesis of Cannabidiol Derivatives
Spatiotemporal Labeling Through Photocatalytic Oxidation of Dihydrotetrazines
Acyl Silanes: The Newest Photoaffinity Labeling Probe
LZ-2112 – A Diterpene that Potentiates Antibiotics
A Dual Inhibitor as a Potential Treatment for Alzheimer’s Disease
Scalable Synthesis of a Payload for Antibody–Drug Conjugate Studies
Sweet Mannose Antibiotic: Stereoselective Synthesis and Stereochemical Assignment of A-94964
Potent Anti-Gastric Cancer Alkaloids from Traditional Medicine
Live-Cell Imaging of Glycosidase Activity Using Bis-Acetal-Based Fluorogenic Probes
Enlightening a Radical: A Convergent Total Synthesis of (+)-Actinobolin and Potent Analogues
Synthesis of the Potent Antibiotic Amycolamicin
First Asymmetric Synthesis of (+)-Thienamycin
Evaluation of Benzopyrrolizidinone Pharmacophores Against NMDA-Induced Nerve Cell Injury
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Issue 05/2022

A Wakeup Call for Exhausted CAR T Cells – Targeted Delivery of an Immune Stimulant
An Alternative Reactivity of Sulfonyl Fluorides
A Testimony of Hergenrother’s Rule
Asymmetric Synthesis of Bioactive Lignans and Enantiomeric Antiviral Activity of Niranthin
Total Synthesis of Two Fusicoccanes Identified Potent Anticancer Activities of a Synthetic Intermediate
A Photoswitchable Butyrylcholinesterase Inhibitor for Investigating Alzheimer’s Disease
Fluorogenic Labeling of Nucleic Acids in Living Cells
Potent and Selective PI3Kδ Inhibitors for the Treatment of Hepatocellular Carcinoma
Synthesis of a Redshifted Photolabile Protecting Group Based on a NIR Dye via a DFT-Based Design
Discovery of Non-Nucleotide STING Agonists
The First Total Synthesis of (±)-Forskolin
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Issue 04/2022

Electrochemical Late-Stage Methylation
Double the Bet: Discovery of Dimeric Cinchona Alkaloid-Inspired Macrocycles as LC3 Lipidation Inducers
A Novel Thiazolidine Scaffold that Inhibits O-GlcNAcase (OGA)
A Sweet Bonus to Drug Release
Structural Diversification of 14-Membered Macrolides
Nitrogen Lovers – Azaphilone Natural Products Inspire the Development of Bioconjugation Reagents
Iridium, Palladium, Cobalt and Rhodium Came to Hamigeran M’s Party
Scalable Synthesis of a Key Fluoro-BPin Fragment towards MCL‑1 Inhibitors
Transition Metal Catalysis Enables an Efficient Synthesis of Soraphen A
SEAKing Cancer Cells to Locally Activate Prodrugs
Late-Stage Photocatalytic C–H Olefination
Photoaffinity Probe Identifies New Cellular Targets of Lenalidomide
A Cyclic Twist: Enantioselective Formation of Spirocyclic Oxindoles via Double Alkylation
Novel Photocleavable Protecting Group for Native Chemical Ligation
Synthesis of Toxicodenane A – A Sesquiterpenoid that Protects Cells from Lipotoxicity
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Issue 03/2022

Process Development for the Synthesis of Hepatitis C NS5A Protein Inhibitor Odalasvir
Convergent Synthesis of the Antibiotic Amycolamicin
Total Synthesis of Sphingofungins A–D within 10 Steps
A Photoredox-Enabled Arene Radiofluorination for PET Imaging
Synthesis of Tricyclic Prostaglandin D2 Metabolite (PGDM) Streamlined by Transition Metal Catalysis
Disruption of LIN28–let-7 Protein–RNA Interaction by Tricyclic Tetrahydroquinolines as an Anticancer Strategy
Regioselective Alkene Diarylation under Catalyst Control
Optimization of a Noncovalent KRASG12D Inhibitor
Structural Mimicry Against Antibiotic Resistance
A Ring-Expansion Strategy Enables the Discovery of Spiro cRAF Inhibitor SHR902275
Synthesis and Antibiotic Activity of Micrococcin P2
Central Nervous System-Penetrant Inhibitors of ELOVL1
CyLBams Enable Analysis of Antibody–Drug Conjugate Linker Chemistry
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Issue 02/2022

An Orally Available Clinical Candidate to Treat Covid-19
Astercins: Sterol-Derived Cholesterol Transport Protein Inhibitors
Identifying the Long Sought-After Ligand of the Sigma-2 Receptor
C-Ar-Nucleosides by Nickel-Catalyzed Reaction
Scratching the Surface of MRGPRX
Photoaffinity Probe Elucidates Mechanism of Action of a COVID-19 Drug Candidate
Uncaging Antisense Oligonucleotides with Small Molecules
Synthesis of (–)-Glionitrin A and B
Carbonyl Transposition Simplifies Synthesis
Sweet Spot: Seneciobipyrrolidine Analogues on Glucose Homeostasis
Benzoxaborole Inhibitor of CPSF3 for the Treatment of Visceral Leishmaniasis
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Issue 01/2022

The Next Generation Lincosamide: Iboxamycin
BromoTag – A ‘Bump-and-Hole’ PROTAC System
Biosynthetic Glycan Labeling
Development of a Selective PI3Kγ Inhibitor
Aristoquinoline – A nAChRally Occurring Antagonist
Glutathione-Sensitive Imaging and Targeted Drug Delivery
Orally Dosed Lipid-Lowering Peptide
Expanding the Toolbox of Synthetic Genetics
Photoswitchable Anion Carriers
Umibecestat, A Highly Selective β‑Secretase (BACE1) Inhibitor
Presaccharothriolide Z, an (E)-Enone-Containing, 10-Membered Macrolactone
No Strain-No Gain: Adducts of Strain-Release Povarov Reaction Against Multidrug-Resistant Persister Bacteria
Hygromycin A Finds a New Purpose
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Issue 12/2021

On-Demand Synthesis of Modified Oligonucleotides
Design and Development of Dual 5-HT3R/5-HT6R Antagonists
Stable Colibactin Analogues Enable Mechanism of Action Studies
Off-Switch Rapamycin
Catalytic eDHFR Acylation in HEK293T Cells
Pyrrole Hemithioindigos: The New Photoswitch on the Block
Straight to the Heart of the Problem: Factor XIa Inhibitor for Antithrombotic Therapy
Assessment of GSK2798745 Metabolite
A Solid Way to Purify Polyethylene Glycols
A Novel Covalent Bruton’s Tyrosine Kinase Inhibitor
KEAP on Searching for Novel E3 Ligases
Wittig Reagents for Sulfenic Acid Ligation
Keep in Mind: An Oxadiazine as Gamma Secretase Modulator for Treating Alzheimer’s Disease
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Issue 11/2021

An Asymmetric [3+2] Cycloaddition/Ring-Expansion Sequence Towards Lysergic Acid
Synthesis of Arimetamycin Hybrids
Concise Synthesis of Deoxygenated Sugar
A Photocatalytic Approach towards Cyclopentanonyl-Fused Cyclic Ethers
Handy Thioethers: Biotin-Derived Sulfimides as Protein and DNA Labeling Tools
4-Aminoquinazolines as Potent Inhibitors of the G Protein-Coupled Receptor Kinase 6 (GRK6)
Discovery of Soticlestat, a Potent and Selective Inhibitor for Cholesterol 24-Hydroxylase (CH24H)
Redirection of the Transcription Factor SP1 by Synthetic Molecules
A Chiral Hydrindane Mimics Fatty Acid and Inhibits ToxT
Taking Bicycles on a New Ride
Fine-Tuning of Acid–Base Equilibria on the Synthesis of the Hexacyclic Core of Palau’amine
Freeze! Put your tRNAs up!
The First Total Synthesis of Lysergic Acid
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Issue 10/2021

Aziridines Cross-Dimerize to Larger N-Heterocycles
Photocatalyzed Site-Selective Tyrosine Bioconjugation
Doubly Caged Puromycin
A Novel P(V)-Based Reagent for Asymmetric Synthesis of Thiophosphoramidates
Eschenmoser Sulfide Contraction in the Synthesis of Kinase Inhibitors
Gram-Scale Synthesis of Iboxamycin
Optical Control of Phosphatidic Acid Signaling
Beating Resistant Plasmodium Parasites with the Antimalarial MMV688533
Potent and Selective Orphan GPCR Agonist for the Treatment of Schizophrenia
Activity-Based Probe for Monitoring Ethylene
Optical Control of Sodium Channels
A Rigid Vitamin Diet: Allenic derivatives of Vitamin D
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Issue 09/2021

X-ray Irradiation Promoted Activation of Prodrugs
Go Bi-Steric for Selectivity
Goyazensolide, a Covalent Importin‑5 (IPO5) Inhibitor
Truncated Mycalolide B Analog to Prevent Cancer Metastasis
Macrodiolide Library Synthesis of cGAS-STING Inhibitors
Spiro-Trycyclic Alkaloids as nAChR Antagonists
Targeting Transcription Factors for Degradation
Fighting Malaria with Endoperoxides
Cyclic Disulfides as Selective Thioredoxin Probes
Total Synthesis of Pyrrolylpyrromethane Alkaloids with Antimalarial Activity
Total Synthesis and Configurational Assignment of Mutanobactin D
Total Synthesis and Structure-Activity Studies of Geodiamolide H
Drugging the Undruggable using Irreversible Covalent K-Ras G12C Inhibitors
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Issue 08/2021

Adding Oxygen with N-Ammonium Ylides
Multiple Macrocyclization Strategies in the Syntheses of Potent Myeloperoxidase (MPO) Inhibitors
Novel Antibiotics by Late-Stage Derivatization of Marketed Fidaxomicin
Antimalarial Heterocycles: Tackling Chloroquine-Resistent Plasmodium falciparum
A Synthetic Diterpene Against Persistent Mycobacteria and Biofilm Formation
Synthesis of Bridged 4′-Thio Nucleic Acid Monomers
Folate-Caged PROTACs Favor Cancer Cells
Sanglifehrins and Analogs: Synthesis and Biological Evaluation of their Immunosuppressive Activity
Identification of ENL YEATS Domain Inhibitors through Cell-Based Drug Discovery with SuFEx
Reducing the Risk of Opioid Misuse
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Issue 07/2021

Spirocyclic Ketone Construction via Semipinacol-Type Rearrangement
Biphenyl Imidazopyridines as a New Scaffold for PD-L1 Inhibitors
Synthesis and Application of the 3-Phosphonofluoresceins
Selective Cannabinoid Type 2 Receptor Antagonists
Watching RNA Do Its Job
Site-Selective LYTACs for Targeted Protein Degradation
Scalable Synthesis of Opioids Enabled by a Palladium-Catalyzed Dearomative Arylation
Small-Molecule Inhibitor of an RNA-Modifying Enzyme for Acute Myeloid Leukemia Treatment
Late-Stage Alkylation of Purine Nucleoside at the C6 Position
Utorubicin: A Novel Anthracycline Cancer Prodrug
Next-Generation Macrolide Antibiotics
Stereostructure–Activity Studies of Spirooliganin
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Issue 06/2021

Seven-Step Synthesis of (–)-Colchicine
Better Photoswitch, Better Photopharmacology
Shocking Selectivity for Hsp90α
Concise Synthesis of the Novel Spliceosome Inhibitor H3B-8800
A Blood-Brain Barrier Penetrant Photooxygenation Catalyst for Aβ Degradation
A Novel APJ Receptor Agonist through SAR Studies
Photocaged Antibiotics
Uncaging Ligands using Bioluminolysis
A Better Version of Rhodamine Voltage Reporter by ‘Trapping‘
Thermal Proteome Profiling Identifies the Target of Indophagolin
Covalent Suppression of the Cellular HDM2/p53 Protein-Protein Interaction using NASA
Late-Stage Radiolabeling Enabled by SuFEx
The Woodwardian Synthesis of Erythromycin A
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Issue 05/2021

Targeted Tumor Therapy via Extracellular Calcification
EC5026, an Analgesic Without the Addictive Potential of Opioids
Synthesis of cis-Aminopiperidine by Asymmetric Hydrogenation
BET Bromodomain Inhibitors Promote Wound Healing
Toward Catalytic Antibiotics
A New Approach for the Synthesis of Covalent Inhibitor Libraries
Discovery of LYS006, an Inhibitor of Leukotriene A4 Hydrolase for the Treatment of Inflammatory Diseases
Targeting Mutant BRAF with PROTACs
Enantioselective Diacetoxylation of Terminal Alkenes
E7766, a Novel Interferon Genes (STING) Agonist
The First Total Synthesis of Cocaine
Synthesis of (±)-Uvaridacol L: An Antiausterity Agent
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Issue 04/2021

Sucrose Analogues for Real-Time Imaging of Intracellular Plant Metabolism
Total Synthesis of Cephalosporin C
Optical Control of the Cannabinoid Receptor 2
Novel Prodrugs for Targeted Cancer Therapy
Light-Induced Cell Cycle Arrest and Apoptosis
A Potent Preclinical Plasmodium Proteasome Inhibitor
Modular Chemoenzymatic Synthesis of GE81112 B1
Diversity-Focused Semisynthesis of Polyether Ionophores with New Antibacterial Selectivity
Evaluation of C2−C2′ Bond Stereochemistry Influence on Cytotoxicity of (–)-Lomaiviticin A
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Issue 03/2021

Lysine-Selective Oxidative Addition Complexes for the Conjugation of Proteins, Antibodies, and Peptides
Selective PI3Kγ Inhibitors for in vivo Studies
Inhibition of Mitochondrial Transcription
A Brain-Penetrant mTOR Kinase Inhibitor for the Treatment of Neurological Disorders
Tabernanthalog, an Ibogaine Analogue for Treatment of Addiction and Depression
Covalent Inhibitors and Fluorescent Probes for Investigation of SARS-CoV-2 Mpro in Patient Samples
PET Imaging of Alzheimer’s Disease With a 64Cu Multivalent Bifunctional Chelator
Pamiparib – A Promising PARP Inhibitor
Styrylbenzothiazoles – A New Class of Photoswitches
A Novel and Highly Selective FAK Inhibitor
Antibiotics in a Trojan Horse
Ratiometric Fluorescent Sensing of Intracellular Potassium
The First Synthesis of Morphine
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Issue 02/2021

RNA-Binding Protein Degradation with PROTACs
Optical Control of CAR-T Cell Function
Cell Type-Selective Secretome Profiling In Vivo
Erythromycin–Fluorophore Conjugates for the Study of Bacterial Resistance Mechanisms in Single-Cells
Three Is All You Need – Photoredox/Nickel-Catalyzed Protocol to Chiral β-Alkyl-α-Arylated Carbonyls
Activity-Based Glycosidase Probes for Tumor Imaging
Non-Enzymatic Phospholipid Synthesis in Water
Muxfeldt’s Synthetic Tetracycline Antibiotics
Development of Small-Molecule ENPP1 Inhibitors
Design and Synthesis of Bryostatin 1 Analogues
1O2 Self-Reporting Photosensitizer for Phototherapy
Dibromoacetone as an Efficient Linker for Protein Ubiquitination
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Issue 01/2021

Teaching Old Clicks New Tricks
Serine-Selective Bioconjugation
Morpholine Analogues of Zampanolide
A Fluorogenic Probe for the Detection of Sphingosine
A Mild Method to Access Various Sulfur(VI)-Fluorides
Selective Electrochemical Benzylic C–H Functionalization
A Protecting Group Orchestration Enables Modular Access to Libraries of Heparan Sulfate Oligosaccharides
A Silicon-Based Pain Killer ‘Sila-Ibuprofen’
Versatile Thermoreversible Nucleic Acid Caging
Bright and Orthogonal NanoLuc Substrates
Sarin and Other G-Series Nerve Agents
Click-Chemistry Based Enrichment Strategy Extends the Detectable Metabolome in LC-HRMS/MS Analysis
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Issue 12/2020

Next Generation Vancomycin Total Synthesis
Introducing a Chiral Tricycle that Renders a Selective JAK Inhibitor
Overcoming Vat Resistance with de Novo Synthesis of New Group A Streptogramin Analogues
Radical Difluorination
Local Labeling of Lipids
Diversity-Oriented Synthesis of Acylphloroglucinol Scaffolds
First Simultaneous Removal of SIRT2 Deacetylase and Defatty-Acylase Activities with PROTACs
A New Generation of Molecular Imaging Probes for Carbon Monoxide Detection in Living Systems
Optical Control of the Peroxisome Proliferator-Activated Receptor γ (PPARγ)
Stereoselective Covalent Inhibitors of T-Cell Activation
Progesterone from Mexican Yams
Sulfuramidimidoyl Fluorides as SuFEx Electrophiles for the Inverse Drug Discovery of Covalent Drugs
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Issue 11/2020

A PROTAC for KRAS G12C Degradation
PEARL-seq: A Workflow for Analyzing Small Molecule–RNA Interactions
Macropinocytosis is Key to Peptidomimetic Uptake in Cancer Cells
Natural Products in Drug Discovery
Copper Sensing by Electrophile Activation
Introducing Phosphorylation-Inducing Chimeric Small Molecules (PHICS)
Non-nucleotide cGAMP Mimetics with Powerful Antitumor Activity
Total Synthetic Lankacidin Antibiotics
A Mild and General Synthesis of Substituted Anilines
A Tool to Observe Cellular Apposition
One, Two, Three – Nucleosides
Bioluminescence Seeing Red
The First Contraceptive
Pumping and Probing for the Optimal Dienophile
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Issue 10/2020

A Long-Lasting HIV-Capsid Inhibitor
Orexin-1-Receptor-Selective Antagonists through Structure-Based Drug Design
Peptide Antagonist of CGRP Receptor for Migraine Treatment
Light-Controlled Carbonation
6-Aza-artemisinins as Potent Antimalarial Drugs
Depalmitoylation Strategy to Inhibit NRAS Signaling
Hapten Deuteration of a Heroin Vaccine
Structural Modification of Oridonin Yields A More Potent Anticancer Agent
Total Synthesis of N14-Desacetoxytubulysin H Using Passerini Multicomponent Reaction (MCR)
Janelia Fluor Photosensitizers
Covalent Inhibitors for PIP Signaling
Maleimides Allow for Cycloaromatization of Acyclic Enediynes
Efficient Total Synthesis of Lipid I and Lipid II Analogues
SYK Inhibitor with Improved hERG-Profile
Dansyl’s First Dance
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Issue 09/2020

Selective Activation of Protein Phosphatase 2A Complexes
Dexamethasone – A Corticosteroid Reduces Death in Severe COVID-19
Design and Synthesis of Antiviral Drug Candidates Targeting SARS-CoV-2 Main Protease
A Potent and Selective Covalent Inhibitor of Pin1
Membrane Photoswitches on Neuronal Fire
SCH79797: A Two-For-One Deal
An Eight-Step Synthesis of Islatravir
Photoredox Conjugate Addition Allows Access to a New Class of LRH-1 Agonists
Cobalt-Catalyzed Asymmetric Hydrogenation of α,β-Unsaturated Acids
The Gram-Negative Upgrade for Ribocil C
A Toxic RNA Makes Its Own Fluorescent Inhibitor
Chemoselective Cross-Coupling Reactions on Pyridine Derivatives
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Issue 08/2020

Covalent Inhibition of Ras G12C with a Stapled Peptidomimetic
Discovery and Characterization of a Diels–Alderase
Discovery of a CNS-Active Inhibitor of NAPE-PLD
Inhibition of the Pentose Phosphate Pathway Reveals its Importance in the Immune Response
Synthetic Cystobactamid Antibiotics With Improved Activities
Visible-Light-Induced Arene Dearomatization Cascades
Two-Stage Photocatalytic Diamination of Alkenes
Taking Two Monopolar Spindle 1 Kinase Inhibitors to Clinical Trials
Synthesis of Azidoribose Probes to Track Ketoamine Adducts
Fluorophores, Get On My Nerves!
Controlling the Actin Cytoskeleton with Light
Discovery and Total Synthesis of Anaenamides A and B
Optical Control of CRAC Channels
Lipid Tails Make the Difference!
Photoinduced Electron Transfer for the Selective Labeling of Tryptophan Residues
Chrysomycin A and Derivatives against Multi-Drug-Resistant Tuberculosis
Protein−Protein Cross-Coupling with an Electrophilic Palladium Reagent
The First SHP2 PROTAC
Synthesis of the First FDA-Approved HIV Protease Inhibitor
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Issue 07/2020

Selectively Binding a Bromodomain
Bicyclic Arginase Inhibitors to Enhance Cancer Immunotherapy
Sterically Shielded Heptamethine Cyanine Dyes with Enhanced Photophysical Properties
DNA-Compatible Cycloadditions for Rapid Library Synthesis
Chemically Induced Vinylphosphonothiolate Electrophiles for Thiol–Thiol Bioconjugations
Optical Control of Gene Silencing by Azobenzene-Modified siRNA
A Nucleolus-Targeted, Photocaged Pt(IV) Prodrug Overcomes Cancer Resistance
Unraveling Masked GPX4 Inhibitors
The First Selective Inhibitor of DCLK-1
How to Overcome Vancomycin Resistance
Total Synthesis of Galactosyl-Queuosine
A Broadly Reactive Covalent Ligand for Glutamates and Aspartates
Chemoselective Methionine Bioconjugation in the Synthesis of Antibody Drug Conjugates (ADCs)
Potent TAS2R8 Antagonists as Bitterness Blockers
Chemically Induced Dimerization
A Photocrosslinkable Mycobacteria Glycolipid Probe
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Issue 06/2020

α-Ketoamide Inhibitors of SARS-CoV-2 Main Protease
Azithromycin – An Antibiotic to Fight COVID-19?
Crystal Structure of the Main Protease of Human Coronavirus NL63
Hydroxychloroquine – An Antimalarial to Fight COVID-19?
C–H Trifluoromethylation Enabled by a Combination of Decatungstate and Copper Catalysis
Irreversible Covalent Inhibition of TrxR1 Prevents STAT3-Dependent Transcription Activation
MicroMap: Precise Proximity Labeling of Cell Surface Proteins
TREK Channel Family Activator for Relief of Pain and Neurogenic Inflammation
Unleashing the Full Power of the Streptavidin–Biotin Technology in Cellular Uptake
Phosphoglycolipids with Immunomodulatory Activity
Photocaged Dopamine Receptor Ligands
A Vincamine-Derived HCRTR2 Agonist Prevents Morphine-Seeking Behavior in Mouse Models
In Vivo Optochemical Control of Glutamate Receptors with Cloaked Glutamates
Accelerating Aiolos Ablation
Clickable UDP-Galactose Analogues
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Issue 05/2020

Reversible Spatiotemporal Control of Induced Protein Degradation by Bistable PhotoPROTACs
Salinipostin A Probe Identifies Potential Antimalarial Protein Targets
PHOTACs Enable Optical Control of Protein Degradation
Water-Soluble Benzene Mimetics
Engelhardt’s Deoxofluorination 60 Years Later
Introducing Phosphatase-Recruiting Chimeras
Poppin’ Open Propellanes
Late-Stage Epoxidation of Geldanamycin with Peptide-Based Organocatalysts
Natural-Product-Inspired Covalent Telomerase Inhibitors
Catching Cathepsin X in the Act
How to Repurpose Sanger’s Reagent as a Photocage
Sulfo-Click Conjugation
Synthesis of Photo-Caged ATP
cGAS/STING Antagonist Discovered in Butenolide Dimer Library
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Issue 04/2020

RIBOTACs – Targeted Degradation of RNA
Stronger Together!
Protein Modification by Cope Rearrangement
Potent and Selective Acid Sphingomyelinase Inhibitors with Antidepressant Activity
Replacing HN3 with Nitromethane for Schmidt-Type Formation of Amides and Nitriles
Lasonolide A is a Prodrug Activated by LDAH, a Serine Hydrolase
PEP-K: A New Reagent for the O-Phosphorylation of Alcohols
Modular, Targeted IDO Inhibitor for Cancer Immunotherapy
A Potential anti-Pertussis Vaccine Based on Lipopolysaccharide Endotoxins of B. pertussis
A Carbapenemase Probe that Switches on the Light
Cyclic Naphthoquinone Imine Based Antagonists of the RIG-I Innate Immune Receptor
Optical Control of CENP-E Function
A Classic Way of Forming Amide Bonds
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Issue 03/2020

A Repurposed Chemotherapy Drug as C1 Synthon
Permeable and Fluorogenic Nanoscopy Probes
A Highly Selective Inhibitor of TBK1/IKKε
Cell-Type-Specific Voltage Imaging Using Covalently Tethered Fluorophores
A Versatile Cellular Target Engagement Probe for MPC2
Natural PDE4 Inhibitor Toddacoumalone
Bioinspired Nucleobase Caging
Investigating TRPA1 Modulation with Noncovalent Piperidine Carboxamide Based Binders
Staudinger Reduction-Activated Lysine for the Control of Protein Subcellular Localization and SUMOylation
Total Synthesis of a Gene
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Issue 02/2020

Caged Aptamers for Improved Cancer Imaging
Sticking a Label on Tyrosine
Refining Selectivity of p38 MAP Kinase Inhibitors
A First-in-Class, Clinically-Relevant Covalent Inhibitor of KRAS(G12C)
DNA-Compatible Conversion of Primary Amines into Azides
Efficient Multigram Synthesis of Dibenzoazacyclooctyne for Strain-Promoted Alkyne–Azide Cycloadditions
Dual Inhibitors of OGG1/NUDT1 for Probing Disease States
Potent and Selective Inhibitors of Kallikrein-Related Peptidase 6
Biosynthetic Engineering of Polyketide Synthase Modules Towards New Enacyloxin Antibiotics
The First FDA-Approved Antibody-Drug Conjugate
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Issue 01/2020

Total Synthesis of Heliolactone and its Biological Evaluation in Plants
Discovery and Synthesis of Monastrol
To Die or Not to Die – Inhibition of Apoptosis
Influenza Drug Evades Resistance
Hindered Dialkyl Ether Synthesis Electrified
Potent and Metabolically Stable Non-Opioid Analgesics
Improved Fluorogenic Dye-Aptamer Module for Live-Cell RNA-Imaging
Taking KRAS Inhibitors to the Clinic
Bicyclic Sultams Made Easy
Enantiomeric Probe Pairs for Ligandable Proteome Mapping
Structure-Guided Design of ABA Receptor Agonists for the Control of Plant Water Use
A Positive Allosteric Modulator of the Human Dopamine D1 Receptor
A Photosensitive Cyclic Acetal Enables Efficient Photo-release of 1,3-Diol 2-Arachidonoylglycerol
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Issue 12/2019

Bifunctional Ligands of K-Ras Prevent the Recruitment of BRAF in vitro
Labeling of Tetrazines with Spatiotemporal Precision
Click Chemistry for the Synthesis of Azides
Agnostic Screening of Sulfonyl Fluoride Fragments to Generate Selective Covalent Inhibitors
Photocontrol of a Membrane Nanopore Forming Protein
Synthesis of Nucleoside Oligophosphates: Quick and Not Dirty
Chemical Microbiology and Synthesis Reveals the Structure of Colibactin and its Mode of Genotoxicity
Merging Indole and Morphan Fragments to Form Potent Glucose Transporter Inhibitors
Functionalization and Post-Translational Modification of Cysteines by Tsuji–Trost Reaction
Versatile One-Step Approach to Caged Fluorophores
Torgov Cyclization
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Issue 11/2019

Water-Soluble BODIPY Dyes for Voltage Imaging
Pre-Exposure Prophylaxis (PrEP)
Sign-Inversion in Photopharmacology
HPLC-Free Synthesis of Nucleoside Triphosphates
Targetable, Bright Small-Molecule Ca2+ Indicators
Macrocycle Library Synthesis through Thiol-to-Amine Cyclization
Membrane Probes for Super-Resolution Imaging of Plasma Membranes
Activatable Photosensitizers for Photodynamic Therapy
C–N Coupling of Aryl Thianthrenium Salts
An Aromatic Brønsted Acid Catalyst for the Direct Glycosylation of Amides
pH-Sensitive μ Opioid Receptor Agonists
Conformational Restricted Cyclopropanated Nucleoside Derivatives
SPiDER-Killer-βGal: A Photosensitizer for Targeted Cell Ablation with Single-Cell Resolution
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Issue 10/2019

Binding-Site Hotspot Mapping using Photochemical Proteomics
Structure-Guided Discovery of Selective Mcl-1 Inhibitors
Ethynylphosphonamidates in the Synthesis of Antibody–Drug Conjugates
A Reagent for Doubly Bioorthogonal Cysteine Labeling
Staudinger Ligation in Living Animals
Photocatalytic Defluoroalkylation of Unactivated Trifluoromethylarenes
Targeted Degradation of Extracellular Proteins with ENDTACs
Profiling of Inhibitor-Bound Kinase Complexes
Selenophosph(V)azanes as Transporters and Sensors
Defying the Odds – Drugging KRAS
In vivo Visualization of Copper(II) in the Brain
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Issue 09/2019

Palladium-Catalyzed Synthesis of Pyrimidine Nucleoside Analogs
Efficient Synthesis of the Heparin Anticoagulant Idraparinux
Late-Stage 18F Incorporation with Photoredox Catalysis
A Small-Molecule Inhibitor of C5 Complement Protein
Synthesis of Fluorinated Nucleoside Analogs with Antiviral Activity
A Sensor for Attomolar Copper Levels
Extreme Sulfur Species Mediate Cellular Uptake
A Fluorescent Probe for Thioredoxin Reductase
The First Total Synthesis of Artemisinin (Qinghaosu)
A Hydrolytically Stable Analog of Decitabine
Visualizing Prostate Cancer with Activatable Fluorophores
Chemical Protein Degradation Targeting Non-Functional Binding Sites
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Issue 08/2019

A Mitochondria-Targeting Calcium Dye
Small-Molecule Inhibitors of CRISPR-Cas9
In Vivo Imaging of Glucose Uptake
Chemical Diversification of Pleuromutilin
Highly Selective Insulin-Degrading Enzyme Inhibitors
Selective α-Glycosidation of Sialic Acid
Short Synthesis of the 3-Deazaguanosine RNA Building Block
SCOTfluors: Small, Conjugatable, Orthogonal, and Tunable Fluorophores
Photoactivated Fluxional Fluorophore Enables Extended Time-Lapse Microscopy
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Issue 07/2019

An in Vivo Mass Cytometry Probe for Protein Translation
Sulfonium Sugars with Antidiabetic Activities
Synthesis of the Smallest Cyclodextrins
Sphingosine-1-phosphate Photopharmacology
Optical Control of Cardiac Function
C–H Activation and Decarboxylative Cross-Coupling of Carboxylic Acids
Targeting Myc through Stabilization of the Max Homodimer
Activity-Based Profiling of Bile Salt Hydrolases
The First Method to Sequence DNA
A Route to Complex N-Arylated Alkylamines via Photocatalytic C–H Amination
Optimizing Triarylborane Fluorophores for Biological Applications
Bioinspired Histidine Bioconjugation
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Issue 06/2019

LYTACs for the Degradation of Secreted and Membrane Proteins
Design and Synthesis of a Selective CDK7 Covalent Inhibitor
Discovery of New Chemotypes by Deep Screening of an Ultra-large Virtual Library
Prebiotic Link between RNA and DNA
Late-Stage Negishi Coupling of Peptides
A Highly Selective and Potent Small-Molecule Inhibitor of Factor B
A Far-Red Emitting IrIII-Complex–Coumarin Dyad for Photodynamic Therapy
Dual Inhibitors of Anaplastic Lymphoma Kinase and Bromodomain‑4
Clickable FPP/GGPP Analogues Enable Analysis of Prenylome
Modification of Phosphinopeptidic Scaffolds by Giese-Type Alkylation
Development of Fluorescent Ca2+ Sensors
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Issue 05/2019

Four New DNA Building Blocks
Organelle-Targeted Membrane Tension Probes
Bioactive Analogues of TAN-2483B
A Manganese-Based Contrast Agent for Imaging Calcium Ions
Functionalization of Palladium Oxidative Addition Complexes Derived From Pharmaceuticals
Targeting the RAS–SOS1 Interaction
Ethynylphosphonamidate-Cysteine Bioconjugation
A High Affinity Fluorescent Sensor for Norepinephrine
Ring-Closing Metathesis in the Synthesis of Simeprevir
Antimalarial 1,2,4-Triazine Dimers
New Methods to Access DNA-Encoded Libraries (DELs)
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Issue 04/2019

A Chemoselective Conjugation of Peptides with Electron-Rich (Hetero)Arenes
Specific Functionalization of Cysteine and Lysine Using Dinitroimidazoles
Late-Stage Functionalization of Complex Primary Sulfonamides via NHC Catalysis
Application of Hemithioindigo Photoswitches in Photopharmacology
Synthesis of Aglaroxin C Analogues for Hepatitis C Viral Infection Inhibition
Synthesis of a cGAMP Analogue
A Small Clickable and Photoconvertible Fluorophore
Synthesis of AWZ1066S, an anti-Wolbachia Drug Candidate
Pyrazolopyrimidines: Molecular Correctors for MALT1-Related Immune Defects
Selective Targeting of p38 MAPK Isoforms Using PROTACs
Synthesis of Human Interleukin-8 by Native Chemical Ligation
Synthesis of a Fluorescent Probe for Cell Surface Phosphatidylserine
Synthesis of ‘Stretched’ Isosteres of Saturated Nitrogen Heterocycles
Targeting Zinc Homeostasis in Cancer
A Glutathione-Labile Oligonucleotide Protecting Group
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Issue 03/2019

A New Class of Stimulator of Interferon Genes Receptor Agonists
Design and Synthesis of a Potent Spongistatin 1 Analogue
Organophotoredox-Catalyzed Sulfoximidation of Electron-Rich Arenes
A Fluorinated Carbocyclic Nucleoside with Anti-HBV Activity
Synthesis, Configuration, and Activity of an Anti-inflammatory Resolving Agonist
Synthesis and Biological Evaluation of Macrocyclic Δ12-Prostaglandin J2 Analogues
A Nimbolide-Derived PROTAC
Copper-Catalyzed ortho-Radiofluorination of Aromatic C–H Bonds
Protecting-Group Free Synthesis of (–)-Δ8-THC Derivatives
Photoswitchable Gramicidin S Derived β‑Hairpin Peptides
Near-IR Polymethine Fluorophores Absorbing Beyond 1000 nm
An Improved Photocaged Puromycin
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