Partially Saturated Bicyclic Heteroaromatics as an sp3 -Enriched Fragment Collection

Design Principles for Fragment Libraries: Maximizing the Value of Learnings from Pharma Fragment-Based Drug Discovery (FBDD) Programs for Use in Academia

(2016) György M. Keserű et al.   JOURNAL OF MEDICINAL CHEMISTRY

Cobalt-Catalyzed Enantioselective Hydrogenation of Minimally Functionalized Alkenes: Isotopic Labeling Provides Insight into the Origin of Stereoselectivity and Alkene Insertion Preferences

(2016) Max R. Friedfeld et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

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

(2016) Nick Palmer et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

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

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

The chemistry of the carbon-transition metal double and triple bond: Annual survey covering the year 2013

(2015) James W. Herndon   COORDINATION CHEMISTRY REVIEWS

Tetrahydroindazoles as Interleukin-2 Inducible T-Cell Kinase Inhibitors. Part II. Second-Generation Analogues with Enhanced Potency, Selectivity, and Pharmacodynamic Modulation in Vivo

(2015) Jason D. Burch et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis of allylated quinolines/isoquinolines via palladium-catalyzed cyclization–allylation of azides and allyl methyl carbonate

(2015) Jiang Luo et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Domino reaction involving the Bestmann–Ohira reagent and α,β-unsaturated aldehydes: efficient synthesis of functionalized pyrazoles

(2015) Shakir Ahamad et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

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

The Use of Chlorobenzene as a Probe Molecule in Molecular Dynamics Simulations

(2014) Yaw Sing Tan et al.   Journal of Chemical Information and Modeling

Fragonomics: The -Omics with Real Impact

(2014) Edward R. Zartler   ACS Medicinal Chemistry Letters

Fragment-based hit identification: thinking in 3D

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

An Approach to 2,4-Substituted Pyrazolo[1,5-a]pyridines and Pyrazolo[1,5-a]azepines by Ring-Closing Metathesis

(2013) Santos Fustero et al.   EUROPEAN JOURNAL OF ORGANIC CHEMISTRY

ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets

(2013) Andrew J Souers et al.   NATURE MEDICINE

Nucleophilic ortho-Allylation of Pyrroles and Pyrazoles: An Accelerated Pummerer/Thio-Claisen Rearrangement Sequence

(2013) Andrew J. Eberhart et al.   ORGANIC LETTERS

Design and synthesis of potent hydroxyethylamine (HEA) BACE-1 inhibitors carrying prime side 4,5,6,7-tetrahydrobenzazole and 4,5,6,7-tetrahydropyridinoazole templates

(2012) Christian Sund et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Reagent-Based DOS: Developing a Diastereoselective Methodology to Access Spirocyclic- and Fused Heterocyclic Ring Systems

(2012) V. Surendra Babu Damerla et al.   Chemistry-An Asian Journal

Enantio- and Regioselective Epoxidation of Olefinic Double Bonds in Quinolones, Pyridones, and Amides Catalyzed by a Ruthenium Porphyrin Catalyst with a Hydrogen Bonding Site

(2012) Philipp Fackler et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

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

A ring-closing metathesis approach to heterocycle-fused azepines

(2012) Thomas A. Moss   TETRAHEDRON LETTERS

Discovery of BMS-846372, a Potent and Orally Active Human CGRP Receptor Antagonist for the Treatment of Migraine

(2012) Guanglin Luo et al.   ACS Medicinal Chemistry Letters

Ligand specificity, privileged substructures and protein druggability from fragment-based screening

(2011) Sarah Barelier et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

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

A Diversity-Oriented Synthesis of Bicycliccis-Dihydroarenediols,cis-4-Hydroxyscytalones, and Bicyclic Conduritol Analogues

(2010) Parag Mukherjee et al.   ORGANIC LETTERS

Synthesis of 3-Chloro-4-fluoro-7,8-dihydro-6H-isoquinolin-5-one and Its Derivatives

(2010) Juraj Velcicky et al.   SYNLETT

Asymmetric catalytic aziridination of dihydronaphthalenes for the preparation of substituted 2-aminotetralins

(2010) Jon Erik Aaseng et al.   TETRAHEDRON

Design and synthesis of orally-active and selective azaindane 5HT2c agonist for the treatment of obesity

(2009) Kevin K.-C. Liu et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

The rise of fragment-based drug discovery

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

A straightforward synthesis of 1,3-dichloro-5,8-dihydroisoquinoline by consecutive Stille cross-coupling and metathesis reactions

(2009) Adri van den Hoogenband et al.   TETRAHEDRON LETTERS

Synthesis of Natural-Product-Like Molecules with Over Eighty Distinct Scaffolds

(2008) Daniel Morton et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Recent Developments in Fragment-Based Drug Discovery

(2008) Miles Congreve et al.   JOURNAL OF MEDICINAL CHEMISTRY