Multicomponent coupling and macrocyclization enabled by Rh(III)-catalyzed dual C–H activation: Macrocyclic oxime inhibitor of influenza H1N1

Marine furanocembranoids-inspired macrocycles enabled by Pd-catalyzed unactivated C(sp3)-H olefination mediated by donor/donor carbenes

(2021) Jiping Hao et al.   Nature Communications

Mechanism-Guided Development of Transition-Metal-Catalyzed C–N Bond-Forming Reactions Using Dioxazolones as the Versatile Amidating Source

(2021) Seung Youn Hong et al.   ACCOUNTS OF CHEMICAL RESEARCH

Use of Strain-Release for the Diastereoselective Construction of Quaternary Carbon Centers

(2021) Tobias Pinkert et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Nitrene-mediated intermolecular N–N coupling for efficient synthesis of hydrazides

(2021) Hao Wang et al.   Nature Chemistry

Zearalenone and the Immune Response

(2021) Cristina Valeria Bulgaru et al.   Toxins

Late-stage C–H functionalization offers new opportunities in drug discovery

(2021) Lucas Guillemard et al.   Nature Reviews Chemistry

Transition-Metal-Catalyzed, Coordination-Assisted Functionalization of Nonactivated C(sp3)–H Bonds

(2021) Bin Liu et al.   CHEMICAL REVIEWS

Pd-Catalyzed Decarboxylative Olefination: Stereoselective Synthesis of Polysubstituted Butadienes and Macrocyclic P-glycoprotein Inhibitors

(2020) Bichao Song et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Evaluation of 3-Dimensionality in Approved and Experimental Drug Space

(2020) Kathleen E. Prosser et al.   ACS Medicinal Chemistry Letters

A modular biomimetic strategy for the synthesis of macrolide P-glycoprotein inhibitors via Rh-catalyzed C-H activation

(2020) Lu Chen et al.   Nature Communications

Dioxazolones: Stable Substrates for the Catalytic Transfer of Acyl Nitrenes

(2020) Kaj M. van Vliet et al.   ACS Catalysis

The rise of molecular simulations in fragment-based drug design (FBDD): an overview

(2020) Maicol Bissaro et al.   DRUG DISCOVERY TODAY

DrugSpaceX: a large screenable and synthetically tractable database extending drug space

(2020) Tianbiao Yang et al.   NUCLEIC ACIDS RESEARCH

Unconventional Macrocyclizations in Natural Product Synthesis

(2020) Iakovos Saridakis et al.   ACS Central Science

Palladium-Catalyzed C(sp3)–H Bond Functionalization of Aliphatic Amines

(2019) Chuan He et al.   Chem

Structure-Based Macrocycle Design in Small-Molecule Drug Discovery and Simple Metrics To Identify Opportunities for Macrocyclization of Small-Molecule Ligands

(2019) Maxwell D. Cummings et al.   JOURNAL OF MEDICINAL CHEMISTRY

Iridium-Catalyzed Enantioselective C(sp3)–H Amidation Controlled by Attractive Noncovalent Interactions

(2019) Hao Wang et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Strategies for the Diversity-Oriented Synthesis of Macrocycles

(2019) Kim T. Mortensen et al.   CHEMICAL REVIEWS

α-Branched amines by catalytic 1,1-addition of C–H bonds and aminating agents to terminal alkenes

(2019) Soham Maity et al.   Nature Catalysis

Synthesis of Biaryl-Bridged Cyclic Peptides via Catalytic Oxidative Cross-Coupling Reactions

(2019) Mor Ben-Lulu et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

A general strategy for synthesis of cyclophane-braced peptide macrocycles via palladium-catalysed intramolecular sp3 C−H arylation

(2018) Xuekai Zhang et al.   Nature Chemistry

Selective formation of γ-lactams via C–H amidation enabled by tailored iridium catalysts

(2018) Seung Youn Hong et al.   SCIENCE

Revisiting Arene C(sp2 )−H Amidation by Intramolecular Transfer of Iridium Nitrenoids: Evidence for a Spirocyclization Pathway

(2018) Yeongyu Hwang et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Backbone-Enabled Directional Peptide Macrocyclization through Late-Stage Palladium-Catalyzed δ-C(sp2 )−H Olefination

(2018) Zengbing Bai et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Chromopynones are pseudo natural product glucose uptake inhibitors targeting glucose transporters GLUT-1 and -3

(2018) George Karageorgis et al.   Nature Chemistry

Rapamycin-inspired macrocycles with new target specificity

(2018) Zufeng Guo et al.   Nature Chemistry

Next Generation of Fluorine-Containing Pharmaceuticals, Compounds Currently in Phase II–III Clinical Trials of Major Pharmaceutical Companies: New Structural Trends and Therapeutic Areas

(2016) Yu Zhou et al.   CHEMICAL REVIEWS

Palladium-Catalyzed Transformations of Alkyl C–H Bonds

(2016) Jian He et al.   CHEMICAL REVIEWS

Twenty years on: the impact of fragments on drug discovery

(2016) Daniel A. Erlanson et al.   NATURE REVIEWS DRUG DISCOVERY

Functionalization of C(sp3)-H bonds using a transient directing group

(2016) F.-L. Zhang et al.   SCIENCE

Rhodium(III)-Catalyzed Amidation of Unactivated C(sp3)H Bonds

(2015) He Wang et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

A diversity-oriented synthesis strategy enabling the combinatorial-type variation of macrocyclic peptidomimetic scaffolds

(2015) Albert Isidro-Llobet et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

A C–H bond activation-based catalytic approach to tetrasubstituted chiral allenes

(2015) Shangze Wu et al.   Nature Communications

New peptide architectures through C–H activation stapling between tryptophan–phenylalanine/tyrosine residues

(2015) Lorena Mendive-Tapia et al.   Nature Communications

Peptide Nanotubes

(2014) Ian W. Hamley   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

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

(2014) André Grossmann et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Macrocyclic Drugs and Synthetic Methodologies toward Macrocycles

(2013) Xufen Yu et al.   MOLECULES

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

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

Peptidic macrocyclization via palladium-catalyzed chemoselective indole C-2 arylation

(2012) Huijun Dong et al.   CHEMICAL COMMUNICATIONS

C–C, C–O and C–N bond formation via rhodium(iii)-catalyzed oxidative C–H activation

(2012) Guoyong Song et al.   CHEMICAL SOCIETY REVIEWS

Gold(I)-Catalyzed Coupling Reactions for the Synthesis of Diverse Small Molecules Using the Build/Couple/Pair Strategy

(2009) Tuoping Luo et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

The rise of fragment-based drug discovery

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

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