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注意：仅列出部分参考文献，下载原文获取全部文献信息。Fragment-to-Lead Medicinal Chemistry Publications in 2020
Iwan J. P. de Esch et al.
JOURNAL OF MEDICINAL CHEMISTRY (2022)
Escape from planarity in fragment-based drug discovery: A physicochemical and 3D property analysis of synthetic 3D fragment libraries
David J. Hamilton et al.
Drug Discovery Today: Technologies (2021)
The Growing Importance of Chirality in 3D Chemical Space Exploration and Modern Drug Discovery Approaches for Hit-ID
Ilaria Proietti Silvestri et al.
ACS MEDICINAL CHEMISTRY LETTERS (2021)
C-H functionalisation tolerant to polar groups could transform fragment-based drug discovery (FBDD)
Gianni Chessari et al.
CHEMICAL SCIENCE (2021)
Emergent synthetic methods for the modular advancement of sp3-rich fragments
Max J. Caplin et al.
CHEMICAL SCIENCE (2021)
Fragment-based drug discovery: opportunities for organic synthesis
Jeffrey D. St Denis et al.
RSC MEDICINAL CHEMISTRY (2021)
The 3F Library: Fluorinated Fsp3-Rich Fragments for Expeditious 19F NMR Based Screening
Nikolaj S. Troelsen et al.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2020)
Discovery of a Covalent Inhibitor of KRASG12C (AMG 510) for the Treatment of Solid Tumors
Brian A. Lanman et al.
JOURNAL OF MEDICINAL CHEMISTRY (2020)
Fragment-to-Lead Medicinal Chemistry Publications in 2018
Daniel A. Erlanson et al.
JOURNAL OF MEDICINAL CHEMISTRY (2020)
Design and Synthesis of 56 Shape-Diverse 3D Fragments
Thomas D. Downes et al.
CHEMISTRY-A EUROPEAN JOURNAL (2020)
Escaping from Flatland: Substituted Bridged Pyrrolidine Fragments with Inherent Three-Dimensional Character
Brian Cox et al.
ACS MEDICINAL CHEMISTRY LETTERS (2020)
Efficient Synthesis of 1,4-Thiazepanones and 1,4-Thiazepanes as 3D Fragments for Screening Libraries
Anil K. Pandey et al.
ORGANIC LETTERS (2020)
Fragment-to-Lead Medicinal Chemistry Publications in 2019
Wolfgang Jahnke et al.
JOURNAL OF MEDICINAL CHEMISTRY (2020)
Demonstration of the utility of DOS-derived fragment libraries for rapid hit derivatisation in a multidirectional fashion
Sarah L. Kidd et al.
CHEMICAL SCIENCE (2020)
Fsp3-rich and diverse fragments inspired by natural products as a collection to enhance fragment-based drug discovery
Abigail R. Hanby et al.
CHEMICAL COMMUNICATIONS (2020)
Construction of a Shape-Diverse Fragment Set: Design, Synthesis and Screen against Aurora-A Kinase
Rong Zhang et al.
CHEMISTRY-A EUROPEAN JOURNAL (2019)
Clinical candidates modulating protein-protein interactions: The fragment-based experience
Dario Valenti et al.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2019)
Spirocycles as Rigidified sp3-Rich Scaffolds for a Fragment Collection
Attila Sveiczer et al.
ORGANIC LETTERS (2019)
Design and Synthesis of Pyrrolidine-based Fragments That Sample Three-dimensional Molecular Space
Philip Garner et al.
ACS MEDICINAL CHEMISTRY LETTERS (2019)
Cycloaddition Strategies for the Synthesis of Diverse Heterocyclic Spirocycles for Fragment-Based Drug Discovery
Thomas A. King et al.
EUROPEAN JOURNAL OF ORGANIC CHEMISTRY (2019)
Evaluating the Advantages of Using 3D-Enriched Fragments for Targeting BET Bromodomains
Jorden A. Johnson et al.
ACS MEDICINAL CHEMISTRY LETTERS (2019)
Discovery of novel Cyclophilin D inhibitors starting from three dimensional fragments with millimolar potencies
Ulrich Graedler et al.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2019)
Design and synthesis of a fragment set based on twisted bicyclic lactams
Haitham Hassan et al.
BIOORGANIC & MEDICINAL CHEMISTRY (2018)
Synthesis of Structurally Diverse N-Substituted Quaternary-Carbon-Containing Small Molecules from α,α-Disubstituted Propargyl Amino Esters
Natalia Mateu et al.
CHEMISTRY-A EUROPEAN JOURNAL (2018)
Synthesis of Enantiomerically Pure 6-Substituted-Piperazine-2-Acetic Acid Esters as Intermediates for Library Production
Srinivas Chamakuri et al.
JOURNAL OF ORGANIC CHEMISTRY (2018)
Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1
Joseph Schoepfer et al.
JOURNAL OF MEDICINAL CHEMISTRY (2018)
Recent Applications of Diversity-Oriented Synthesis Toward Novel, 3-Dimensional Fragment Collections
Sarah L. Kidd et al.
FRONTIERS IN CHEMISTRY (2018)
Current perspectives in fragment-based lead discovery (FBLD)
Bas Lamoree et al.
STRUCTURE-BASED DRUG DESIGN: INSIGHTS FROM ACADEMIA AND INDUSTRY (2017)
Divergent Synthesis of Cyclopropane-Containing Lead-Like Compounds, Fragments and Building Blocks through a Cobalt Catalyzed Cyclopropanation of Phenyl Vinyl Sulfide
Stephen J. Chawner et al.
EUROPEAN JOURNAL OF ORGANIC CHEMISTRY (2017)
Construction of a 3D-shaped, natural product like fragment library by fragmentation and diversification of natural products
Horst Prescher et al.
BIOORGANIC & MEDICINAL CHEMISTRY (2017)
Opportunity Knocks: Organic Chemistry for Fragment-Based Drug Discovery (FBDD)
Christopher W. Murray et al.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2016)
Partially Saturated Bicyclic Heteroaromatics as an sp3-Enriched Fragment Collection
David G. Twigg et al.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2016)
An improved model for fragment-based lead generation at AstraZeneca
Nathan Fuller et al.
DRUG DISCOVERY TODAY (2016)
The discovery of vemurafenib for the treatment of BRAF-mutated metastatic melanoma
Alex Kim et al.
EXPERT OPINION ON DRUG DISCOVERY (2016)
Design and synthesis of dihydroisoquinolones for fragment-based drug discovery (FBDD)
Nick Palmer et al.
ORGANIC & BIOMOLECULAR CHEMISTRY (2016)
Microwave-assisted synthesis of functionalized spirohydantoins as 3-D privileged fragments for scouting the chemical space
Hugues Prevet et al.
TETRAHEDRON LETTERS (2016)
Diversity-Oriented Synthesis as a Strategy for Fragment Evolution against GSK3β
Yikai Wang et al.
ACS MEDICINAL CHEMISTRY LETTERS (2016)
A systematic approach to diverse, lead-like scaffolds from α,α-disubstituted amino acids
Daniel J. Foley et al.
CHEMICAL COMMUNICATIONS (2015)
Structure-Guided Blockade of CSF1R Kinase in Tenosynovial Giant-Cell Tumor
W. D. Tap et al.
NEW ENGLAND JOURNAL OF MEDICINE (2015)
Studies on the synthesis, stability and conformation of 2-sulfonyl-oxetane fragments
K. F. Morgan et al.
ORGANIC & BIOMOLECULAR CHEMISTRY (2015)
Synthesis of functionalized 2-isoxazolines as three-dimensional fragments for fragment-based drug discovery
Ngoc Chau Tran et al.
TETRAHEDRON LETTERS (2015)
2-(Aryl-sulfonyl)oxetanes as designer 3-dimensional fragments for fragment screening: synthesis and strategies for functionalisation
Kate F. Morgan et al.
CHEMICAL COMMUNICATIONS (2014)
Efficient exploration of chemical space by fragment-based screening
Richard J. Hall et al.
PROGRESS IN BIOPHYSICS & MOLECULAR BIOLOGY (2014)
Stabilization and Inhibition of Protein Protein Interactions: The 14-3-3 Case Study
Lech-Gustav Milroy et al.
ACS CHEMICAL BIOLOGY (2013)
Fragment-based hit identification: thinking in 3D
Andrew D. Morley et al.
DRUG DISCOVERY TODAY (2013)
Copper-Catalyzed N-Arylation of 2-Imidazolines with Aryl Iodides
Owen A. Davis et al.
JOURNAL OF ORGANIC CHEMISTRY (2013)
Natural-product-derived fragments for fragment-based ligand discovery
Bjoern Over et al.
NATURE CHEMISTRY (2013)
ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets
Andrew J. Souers et al.
NATURE MEDICINE (2013)
Design and pharmacology of a highly specific dual FMS and KIT kinase inhibitor
Chao Zhang et al.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2013)
Escape from Flatland 2: complexity and promiscuity
Frank Lovering
MEDCHEMCOMM (2013)
Plane of Best Fit: A Novel Method to Characterize the Three-Dimensionality of Molecules
Nicholas C. Firth et al.
JOURNAL OF CHEMICAL INFORMATION AND MODELING (2012)
Vemurafenib: the first drug approved for BRAF-mutant cancer
Gideon Bollag et al.
NATURE REVIEWS DRUG DISCOVERY (2012)
Rhodium(III)-Catalyzed Heterocycle Synthesis Using an Internal Oxidant: Improved Reactivity and Mechanistic Studies
Nicolas Guimond et al.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2011)
Route to three-dimensional fragments using diversity-oriented synthesis
Alvin W. Hung et al.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2011)
Escape from Flatland: Increasing Saturation as an Approach to Improving Clinical Success
Frank Lovering et al.
JOURNAL OF MEDICINAL CHEMISTRY (2009)
A planning strategy for diversity-oriented synthesis
MD Burke et al.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2004)
Molecular shape diversity of combinatorial libraries: A prerequisite for broad bioactivity
WHB Sauer et al.
JOURNAL OF CHEMICAL INFORMATION AND COMPUTER SCIENCES (2003)
Prediction of aqueous solubility of organic compounds based on a 3D structure representation
AX Yan et al.
JOURNAL OF CHEMICAL INFORMATION AND COMPUTER SCIENCES (2003)
Molecular complexity and its impact on the probability of finding leads for drug discovery
MM Hann et al.
JOURNAL OF CHEMICAL INFORMATION AND COMPUTER SCIENCES (2001)
Target-oriented and diversity-oriented organic synthesis in drug discovery
SL Schreiber
SCIENCE (2000)
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