Diversity-Oriented Synthesis of Drug-Like Macrocyclic Scaffolds Using an Orthogonal Organo- and Metal Catalysis Strategy

Diversity-oriented synthesis as a tool for identifying new modulators of mitosis

(2014) Brett M. Ibbeson et al.   Nature Communications

Metal and carbene organocatalytic relay activation of alkynes for stereoselective reactions

(2014) Kayambu Namitharan et al.   Nature Communications

N-Heterocyclic-Carbene-Catalyzed One-Pot Synthesis of Hydroxamic Esters

(2013) Xiaoxiao Song et al.   Chemistry-An Asian Journal

A strategy for the diversity-oriented synthesis of macrocyclic scaffolds using multidimensional coupling

(2013) Henning S. G. Beckmann et al.   Nature Chemistry

Exploiting Acyl and Enol Azolium Intermediates via N-Hetero- cyclic Carbene-Catalyzed Reactions of α-Reducible Aldehydes

(2012) Harit U. Vora et al.   ADVANCED SYNTHESIS & CATALYSIS

N-Heterocyclic Carbene Catalyzed Homoenolate-Addition Reaction of Enals and Nitroalkenes: Asymmetric Synthesis of 5-Carbon-Synthon δ-Nitroesters

(2012) Biswajit Maji et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Catalytic Dynamic Kinetic Resolutions with N-Heterocyclic Carbenes: Asymmetric Synthesis of Highly Substituted β-Lactones

(2012) Daniel T. Cohen et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Catalytic Asymmetric Intermolecular Stetter Reactions of Enolizable Aldehydes with Nitrostyrenes: Computational Study Provides Insight into the Success of the Catalyst

(2012) Daniel A. DiRocco et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Macrocycles in new drug discovery

(2012) Jamie Mallinson et al.   Future Medicinal Chemistry

Enumeration of 166 Billion Organic Small Molecules in the Chemical Universe Database GDB-17

(2012) Lars Ruddigkeit et al.   Journal of Chemical Information and Modeling

Biomimetic diversity-oriented synthesis of benzannulated medium rings via ring expansion

(2012) Renato A Bauer et al.   Nature Chemical Biology

A diversity-oriented synthesis approach to macrocycles via oxidative ring expansion

(2012) Felix Kopp et al.   Nature Chemical Biology

A two-directional strategy for the diversity-oriented synthesis of macrocyclic scaffolds

(2012) Kieron M. G. O'Connell et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

N-Heterocyclic carbene catalyzed synthesis of oxime esters

(2012) Dieter Enders et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Highly Enantioselective Addition of Enals to Isatin-Derived Ketimines Catalyzed by N-Heterocyclic Carbenes: Synthesis of Spirocyclic γ-Lactams

(2012) Hui Lv et al.   ORGANIC LETTERS

Extending NHC-Catalysis: Coupling Aldehydes with Unconventional Reaction Partners

(2011) Akkattu T. Biju et al.   ACCOUNTS OF CHEMICAL RESEARCH

Lewis Acid Activated Synthesis of Highly Substituted Cyclopentanes by the N-Heterocyclic Carbene Catalyzed Addition of Homoenolate Equivalents to Unsaturated Ketoesters

(2011) Daniel T. Cohen et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Merging Metal and N-Heterocyclic Carbene Catalysis: On the Way to Discovering Enantioselective Organic Transformations

(2011) Nitin T. Patil   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Enantioselective Stetter Reactions of Enals and Modified Chalcones Catalyzed by N-Heterocyclic Carbenes

(2011) Xinqiang Fang et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Highly Enantioselective Synthesis of α-Amino Acid Derivatives by an NHC-Catalyzed Intermolecular Stetter Reaction

(2011) Thierry Jousseaume et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Biology-Oriented Synthesis

(2011) Stefan Wetzel et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

N-Heterocyclic Carbene Catalyzed Domino Reactions

(2011) André Grossmann et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

A Simple Recipe for Sophisticated Cocktails: Organocatalytic One-Pot Reactions-Concept, Nomenclature, and Future Perspectives

(2011) Łukasz Albrecht et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Strategies to improve in vivo toxicology outcomes for basic candidate drug molecules

(2011) Tim Luker et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

A design strategy for drug-like polyheterocycles with privileged substructures for discovery of specific small-molecule modulators

(2011) Sangmi Oh et al.   CHEMICAL COMMUNICATIONS

Chemical genetics

(2011) Cornelius J. O' Connor et al.   CHEMICAL SOCIETY REVIEWS

Employing homoenolates generated by NHC catalysis in carbon–carbon bond-forming reactions: state of the art

(2011) Vijay Nair et al.   CHEMICAL SOCIETY REVIEWS

Mechanistic Insights on N-Heterocyclic Carbene-Catalyzed Annulations: The Role of Base-Assisted Proton Transfers

(2011) Pragya Verma et al.   JOURNAL OF ORGANIC CHEMISTRY

Catalytic Asymmetric Intermolecular Stetter Reaction of Enals with Nitroalkenes: Enhancement of Catalytic Efficiency through Bifunctional Additives

(2011) Daniel A. DiRocco et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Natural product–inspired cascade synthesis yields modulators of centrosome integrity

(2011) Heiko Dückert et al.   Nature Chemical Biology

Contemporary strategies for peptide macrocyclization

(2011) Christopher J. White et al.   Nature Chemistry

Fragment-based domain shuffling approach for the synthesis of pyran-based macrocycles

(2011) E. Comer et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Diversity-oriented synthesis of macrocyclic peptidomimetics

(2011) A. Isidro-Llobet et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Cooperative Lewis acid/N-heterocyclic carbene catalysis

(2011) Daniel T. Cohen et al.   Chemical Science

Diversity-Oriented Synthesis Yields a Novel Lead for the Treatment of Malaria

(2011) Richard W. Heidebrecht et al.   ACS Medicinal Chemistry Letters

α-Aroyloxyaldehydes: scope and limitations as alternatives to α-haloaldehydes for NHC-catalysed redox transformations

(2010) Kenneth B. Ling et al.   CHEMICAL COMMUNICATIONS

Peptoid Macrocycles: Making the Rounds with Peptidomimetic Oligomers

(2010) Barney Yoo et al.   CHEMISTRY-A EUROPEAN JOURNAL

CooperativeN-Heterocyclic Carbene/Lewis Acid Catalysis for Highly Stereoselective Annulation Reactions with Homoenolates

(2010) Benoit Cardinal-David et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

An Aldol-Based Build/Couple/Pair Strategy for the Synthesis of Medium- and Large-Sized Rings: Discovery of Macrocyclic Histone Deacetylase Inhibitors

(2010) Lisa A. Marcaurelle et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

An Enantioselective Claisen Rearrangement Catalyzed by N-Heterocyclic Carbenes

(2010) Juthanat Kaeobamrung et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Cooperative catalysis by carbenes and Lewis acids in a highly stereoselective route to γ-lactams

(2010) Dustin E. A. Raup et al.   Nature Chemistry

Highly enantioselective synthesis and cellular evaluation of spirooxindoles inspired by natural products

(2010) Andrey P. Antonchick et al.   Nature Chemistry

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

Multicatalytic, asymmetric Michael/Stetter reaction of salicylaldehydes and activated alkynes

(2010) C. M. Filloux et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Diversity-oriented synthesis as a tool for the discovery of novel biologically active small molecules

(2010) Warren R.J.D. Galloway et al.   Nature Communications

The discovery of antibacterial agents using diversity-oriented synthesis

(2009) Warren R. J. D. Galloway et al.   CHEMICAL COMMUNICATIONS

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

Is synthesis the main hurdle for the generation of diversity in compound libraries for screening?

(2009) Warren RJD Galloway et al.   Expert Opinion on Drug Discovery

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

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

Highly Enantioselective Benzoin Condensation Reactions Involving a Bifunctional Protic Pentafluorophenyl-Substituted Triazolium Precatalyst

(2009) Louise Baragwanath et al.   JOURNAL OF ORGANIC CHEMISTRY

Asymmetric Synthesis of Functionalized Cyclopentanones via a Multicatalytic Secondary Amine/N-Heterocyclic Carbene Catalyzed Cascade Sequence

(2009) Stephen P. Lathrop et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Catalytic Asymmetric Intermolecular Stetter Reaction of Heterocyclic Aldehydes with Nitroalkenes: Backbone Fluorination Improves Selectivity

(2009) Daniel A. DiRocco et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

A small molecule that binds Hedgehog and blocks its signaling in human cells

(2009) Benjamin Z Stanton et al.   Nature Chemical Biology

Enantio- and Diastereoselective Intermolecular Stetter Reaction of Glyoxamide and Alkylidene Ketoamides

(2009) Qin Liu et al.   ORGANIC LETTERS

Novel Nucleophilic Heterocyclic Carbene Mediated Stereoselective Conjugate Addition of Enals to Nitrostyrenes via Homoenolate§

(2009) Vijay Nair et al.   ORGANIC LETTERS

From Mono-Triazolium Salt to Bis-Triazolium Salt: Improvement of the Asymmetric Intermolecular Benzoin Condensation

(2008) Yajun Ma et al.   ADVANCED SYNTHESIS & CATALYSIS

Anti-MRSA Agent Discovery Using Diversity-Oriented Synthesis

(2008) Gemma L. Thomas et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Biology-inspired synthesis of compound libraries

(2008) M. Kaiser et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

Asymmetric intermolecular Stetter reactions catalyzed by a novel triazolium derived N-heterocyclic carbene

(2008) Dieter Enders et al.   CHEMICAL COMMUNICATIONS

Catalytic Asymmetric Intermolecular Stetter Reaction of Glyoxamides with Alkylidenemalonates

(2008) Qin Liu et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

The exploration of macrocycles for drug discovery — an underexploited structural class

(2008) Edward M. Driggers et al.   NATURE REVIEWS DRUG DISCOVERY

Towards the Optimal Screening Collection: A Synthesis Strategy

(2007) Thomas E. Nielsen et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION