Design and synthesis of dihydroisoquinolones for fragment-based drug discovery (FBDD)

Opportunity Knocks: Organic Chemistry for Fragment-Based Drug Discovery (FBDD)

(2015) Christopher W. Murray et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Progress in discovery of small-molecule modulators of protein–protein interactions via fragment screening

(2015) Thomas V. Magee   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of Tricyclic Indoles That Potently Inhibit Mcl-1 Using Fragment-Based Methods and Structure-Based Design

(2015) Jason P. Burke et al.   JOURNAL OF MEDICINAL CHEMISTRY

Rhodium-catalyzed C–H functionalization-based approach to eight-membered lactams

(2015) Shangze Wu et al.   Chemical Science

Ligand design for Rh(iii)-catalyzed C–H activation: an unsymmetrical cyclopentadienyl group enables a regioselective synthesis of dihydroisoquinolones

(2015) Todd K. Hyster et al.   Chemical Science

Asymmetric Synthesis of Isoindolones by Chiral Cyclopentadienyl-Rhodium(III)-Catalyzed CH Functionalizations

(2014) Baihua Ye et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Rhodium(III)-Catalyzed C–H Activation/Annulation with Vinyl Esters as an Acetylene Equivalent

(2014) Nicola J. Webb et al.   ORGANIC LETTERS

Fragonomics: The -Omics with Real Impact

(2014) Edward R. Zartler   ACS Medicinal Chemistry Letters

Learning from our mistakes: The ‘unknown knowns’ in fragment screening

(2013) Ben J. Davis et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Fragment-based hit identification: thinking in 3D

(2013) Andrew D. Morley et al.   DRUG DISCOVERY TODAY

Rh(III)-Catalyzed C–H Activation and Double Directing Group Strategy for the Regioselective Synthesis of Naphthyridinones

(2013) John R. Huckins et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

The 'rule of three' for fragment-based drug discovery: where are we now?

(2013) Harren Jhoti et al.   NATURE REVIEWS DRUG DISCOVERY

Complementary Regioselectivity in Rh(III)-Catalyzed Insertions of Potassium Vinyltrifluoroborate via C–H Activation: Preparation and Use of 4-Trifluoroboratotetrahydroisoquinolones

(2013) Marc Presset et al.   ORGANIC LETTERS

Lead-Oriented Synthesis: A New Opportunity for Synthetic Chemistry

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

Vemurafenib: the first drug approved for BRAF-mutant cancer

(2012) Gideon Bollag et al.   NATURE REVIEWS DRUG DISCOVERY

Fragment-based lead discovery grows up

(2012) Monya Baker   NATURE REVIEWS DRUG DISCOVERY

Biotinylated Rh(III) Complexes in Engineered Streptavidin for Accelerated Asymmetric C-H Activation

(2012) T. K. Hyster et al.   SCIENCE

Chiral Cyclopentadienyl Ligands as Stereocontrolling Element in Asymmetric C-H Functionalization

(2012) B. Ye et al.   SCIENCE

Molecular complexity and fragment-based drug discovery: ten years on

(2011) Andrew R Leach et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Design of a multi-purpose fragment screening library using molecular complexity and orthogonal diversity metrics

(2011) Wan F. Lau et al.   JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN

Rh(III)-Catalyzed Directed C−H Olefination Using an Oxidizing Directing Group: Mild, Efficient, and Versatile

(2011) Souvik Rakshit et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Rhodium(III)-Catalyzed Heterocycle Synthesis Using an Internal Oxidant: Improved Reactivity and Mechanistic Studies

(2011) Nicolas Guimond et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Design, Synthesis, and In Vitro Evaluation of Potential West Nile Virus Protease Inhibitors Based on the 1-Oxo-1,2,3,4-tetrahydroisoquinoline and 1-Oxo-1,2-dihydroisoquinoline Scaffolds

(2010) Dengfeng Dou et al.   JOURNAL OF COMBINATORIAL CHEMISTRY

Rhodium(III)-Catalyzed Isoquinolone Synthesis: The N−O Bond as a Handle for C−N Bond Formation and Catalyst Turnover

(2010) Nicolas Guimond et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

NMR quantification using an artificial signal

(2010) Roger D. Farrant et al.   MAGNETIC RESONANCE IN CHEMISTRY

Design of compound libraries for fragment screening

(2009) Niklas Blomberg et al.   JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN

The rise of fragment-based drug discovery

(2009) Christopher W. Murray et al.   Nature Chemistry

N-Amidation by Copper-Mediated Cross-Coupling of Organostannanes or Boronic Acids withO-Acetyl Hydroxamic Acids

(2008) Zhihui Zhang et al.   ORGANIC LETTERS