Saturated Heterocyclic Aminosulfonyl Fluorides: New Scaffolds for Protecting-Group-Free Synthesis of Sulfonamides

A metal-free and regioselective approach to ( Z )-β-fluorovinyl sulfones and their chemoselective hydrogenation to β-fluoroalkyl sulfones

(2018) Daniel M. Sedgwick et al.   JOURNAL OF FLUORINE CHEMISTRY

Antibacterial and β-Lactamase Inhibitory Activity of Monocyclic β-Lactams

(2017) Lena Decuyper et al.   MEDICINAL RESEARCH REVIEWS

Functionalized Dialdehydes as Promising Scaffolds for Access to Heterocycles and β-Amino Acids: Synthesis of Fluorinated Piperidine and Azepane Derivatives

(2017) Ferenc Fülöp et al.   SYNTHESIS-STUTTGART

Microwave-enhanced Friedländer synthesis for the rapid assembly of halogenated quinolines with antibacterial and biofilm eradication activities against drug resistant and tolerant bacteria

(2017) Aaron T. Garrison et al.   MedChemComm

Proteasome inhibition by new dual warhead containing peptido vinyl sulfonyl fluorides

(2016) Arwin J. Brouwer et al.   BIOORGANIC & MEDICINAL CHEMISTRY

A divergent synthetic approach to diverse molecular scaffolds: assessment of lead-likeness using LLAMA, an open-access computational tool

(2016) Ignacio Colomer et al.   CHEMICAL COMMUNICATIONS

Improving Drug Design: An Update on Recent Applications of Efficiency Metrics, Strategies for Replacing Problematic Elements, and Compounds in Nontraditional Drug Space

(2016) Nicholas A. Meanwell   CHEMICAL RESEARCH IN TOXICOLOGY

Asymmetric Hydrogenation of Unprotected Indoles Catalyzed by η6-Arene/N-Me-sulfonyldiamine–Ru(II) Complexes

(2016) Taichiro Touge et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Asymmetric Total Synthesis of (−)-Lycospidine A

(2016) Shiyan Xu et al.   ORGANIC LETTERS

Deployment of Small-Ring Azaheterocycles as Building Blocks for the Synthesis of Organofluorine Compounds

(2016) Norbert De Kimpe et al.   SYNLETT

Substrate-dependent fluorinations of highly functionalized cycloalkanes

(2016) Loránd Kiss et al.   TETRAHEDRON

Collective formal synthesis of (±)-rhynchophylline and homologues

(2016) Jun Xu et al.   RSC Advances

A systematic approach to diverse, lead-like scaffolds from α,α-disubstituted amino acids

(2015) Daniel J. Foley et al.   CHEMICAL COMMUNICATIONS

Increasing the delivery of next generation therapeutics from high throughput screening libraries

(2015) Mark J Wigglesworth et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

A Survey of the Role of Noncovalent Sulfur Interactions in Drug Design

(2015) Brett R. Beno et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Synthesis of Alkyl and (Hetero)aryl Sulfonamides From Sulfamoyl Inner Salts

(2015) Joseph M. Young et al.   JOURNAL OF ORGANIC CHEMISTRY

Know your target, know your molecule

(2015) Mark E Bunnage et al.   Nature Chemical Biology

SureChEMBL: a large-scale, chemically annotated patent document database

(2015) George Papadatos et al.   NUCLEIC ACIDS RESEARCH

A unified lead-oriented synthesis of over fifty molecular scaffolds

(2015) Richard G. Doveston et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Sulfonyl fluorides as privileged warheads in chemical biology

(2015) Arjun Narayanan et al.   Chemical Science

SAR Exploration Guided by LE and Fsp3: Discovery of a Selective and Orally Efficacious RORγ Inhibitor

(2015) Kazuyuki Hirata et al.   ACS Medicinal Chemistry Letters

Selective Access to Heterocyclic Sulfonamides and Sulfonyl Fluorides via a Parallel Medicinal Chemistry Enabled Method

(2015) Joseph W. Tucker et al.   ACS Combinatorial Science

Sulfur(VI) Fluoride Exchange (SuFEx): Another Good Reaction for Click Chemistry

(2014) Jiajia Dong et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Selective Inhibition of the Immunoproteasome by Ligand-Induced Crosslinking of the Active Site

(2014) Christian Dubiella et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Olefin Metathesis Reactions with Fluorinated Substrates, Catalysts, and Solvents

(2014) Santos Fustero et al.   CHEMICAL REVIEWS

Sulfonyl Fluorides as Alternative to Sulfonyl Chlorides in Parallel Synthesis of Aliphatic Sulfonamides

(2014) Andrey V. Bogolubsky et al.   ACS Combinatorial Science

Target validation using chemical probes

(2013) Mark E Bunnage et al.   Nature Chemical Biology

DrugBank 4.0: shedding new light on drug metabolism

(2013) Vivian Law et al.   NUCLEIC ACIDS RESEARCH

Lead-Oriented Synthesis: A New Opportunity for Synthetic Chemistry

(2012) Alan Nadin et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Escape from Flatland 2: complexity and promiscuity

(2012) Frank Lovering   MedChemComm

Synthesis and biological evaluation of novel irreversible serine protease inhibitors using amino acid based sulfonyl fluorides as an electrophilic trap

(2011) Arwin J. Brouwer et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Improvement in Aqueous Solubility in Small Molecule Drug Discovery Programs by Disruption of Molecular Planarity and Symmetry

(2011) Minoru Ishikawa et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synopsis of Some Recent Tactical Application of Bioisosteres in Drug Design

(2011) Nicholas A. Meanwell   JOURNAL OF MEDICINAL CHEMISTRY

ChEMBL: a large-scale bioactivity database for drug discovery

(2011) A. Gaulton et al.   NUCLEIC ACIDS RESEARCH

The impact of aromatic ring count on compound developability: further insights by examining carbo- and hetero-aromatic and -aliphatic ring types

(2010) Timothy J. Ritchie et al.   DRUG DISCOVERY TODAY

Grand Challenge Commentary: Accessing new chemical space for 'undruggable' targets

(2010) Sivaraman Dandapani et al.   Nature Chemical Biology

Small molecules of different origins have distinct distributions of structural complexity that correlate with protein-binding profiles

(2010) P. A. Clemons et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Defining optimum lipophilicity and molecular weight ranges for drug candidates—Molecular weight dependent lower logD limits based on permeability

(2009) Michael J. Waring   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

A Practical Method for Targeted Library Design Balancing Lead-like Properties with Diversity

(2009) Michael J. Stocks et al.   ChemMedChem

The impact of aromatic ring count on compound developability – are too many aromatic rings a liability in drug design?

(2009) Timothy J. Ritchie et al.   DRUG DISCOVERY TODAY

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

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

Synthesis of β-aminoethanesulfonyl fluorides or 2-substituted taurine sulfonyl fluorides as potential protease inhibitors

(2009) Arwin J. Brouwer et al.   TETRAHEDRON LETTERS