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

A Concise and Scalable Strategy for the Total Synthesis of Dictyodendrin B Based on Sequential CH Functionalization

(2015) Andrew K. Pitts et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Late-Stage Fluorination: Fancy Novelty or Useful Tool?

(2015) Constanze N. Neumann 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

Fragment-Based Drug Discovery Targeting Inhibitor of Apoptosis Proteins: Discovery of a Non-Alanine Lead Series with Dual Activity Against cIAP1 and XIAP

(2015) Gianni Chessari et al.   JOURNAL OF MEDICINAL CHEMISTRY

Applying thermodynamic profiling in lead finding and optimization

(2015) Gerhard Klebe   NATURE REVIEWS DRUG DISCOVERY

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

The role of ligand efficiency metrics in drug discovery

(2014) Andrew L. Hopkins et al.   NATURE REVIEWS DRUG DISCOVERY

Efficient exploration of chemical space by fragment-based screening

(2014) Richard J. Hall et al.   PROGRESS IN BIOPHYSICS & MOLECULAR BIOLOGY

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

Inhibitors of BACE for treating Alzheimer's disease: a fragment-based drug discovery story

(2013) Andrew Stamford et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Fragment-based hit identification: thinking in 3D

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

De Novo Fragment Design: A Medicinal Chemistry Approach to Fragment-Based Lead Generation

(2013) Francisco X. Talamas et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

Lead-Oriented Synthesis: A New Opportunity for Synthetic Chemistry

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

Natural-product-derived fragments for fragment-based ligand discovery

(2012) Björn Over et al.   Nature Chemistry

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

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

The Medicinal Chemist’s Toolbox: An Analysis of Reactions Used in the Pursuit of Drug Candidates

(2011) Stephen D. Roughley et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

Drug discovery: A question of library design

(2011) Philip J. Hajduk et al.   NATURE

Route to three-dimensional fragments using diversity-oriented synthesis

(2011) A. W. Hung et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Factors Determining the Selection of Organic Reactions by Medicinal Chemists and the Use of These Reactions in Arrays (Small Focused Libraries)

(2010) Tony W. J. Cooper et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Fragment-Based Drug Discovery Applied to Hsp90. Discovery of Two Lead Series with High Ligand Efficiency

(2010) Christopher W. Murray et al.   JOURNAL OF MEDICINAL CHEMISTRY

Kinase-targeted libraries: The design and synthesis of novel, potent, and selective kinase inhibitors

(2009) Irini Akritopoulou-Zanze et al.   DRUG DISCOVERY TODAY

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

Identification ofN-(4-Piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide (AT7519), a Novel Cyclin Dependent Kinase Inhibitor Using Fragment-Based X-Ray Crystallography and Structure Based Drug Design†

(2008) Paul G. Wyatt et al.   JOURNAL OF MEDICINAL CHEMISTRY