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The exploration of macrocycles for drug discovery — an underexploited structural class
1 of 96 checkable references need attention · checked 2026-07-22
At the dated check, the references listed below either did not resolve in Crossref or DataCite, or carried a retraction notice. Each one is shown with the registry record that put it there.
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References needing attention
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The 95 checked references that resolve
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From Protein Domains to Drug CandidatesâNatural Products as Guiding Principles in the Design and Synthesis of Compound Libraries
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What can a chemist learn from nature?s macrocycles? ? A brief, conceptual view
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Discovery of Cyclotide-Like Protein Sequences in Graminaceous Crop Plants: Ancestral Precursors of Circular Proteins?
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A Common Protein Fold Topology Shared by Flavonoid Biosynthetic Enzymes and Therapeutic Targets
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Species-Specific Secondary Metabolite Production in Marine Actinomycetes of the Genus
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Genome sequencing reveals complex secondary metabolome in the marine actinomycete
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Discovery of a New Source of Rifamycin Antibiotics in Marine Sponge Actinobacteria by Phylogenetic Prediction
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Structure of the FKBP12-Rapamycin Complex Interacting with Binding Domain of Human FRAP
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Tacrolimus and pimecrolimus: From clever prokaryotes to inhibiting calcineurin and treating atopic dermatitis
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Natural products to drugs: natural product derived compounds in clinical trials
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Immunophilin-sensitive protein phosphatase action in cell signaling pathways
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Epothilones as Lead Structures for the Synthesis-Based Discovery of New Chemotypes for Microtubule Stabilization
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Tubulin Assembly, Taxoid Site Binding, and Cellular Effects of the Microtubule-Stabilizing Agent Dictyostatin
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Synergistic Effects of Peloruside A and Laulimalide with Taxoid Site Drugs, but Not with Each Other, on Tubulin Assembly
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Comparison of the Activities of the Truncated Halichondrin B Analog NSC 707389 (E7389) with Those of the Parent Compound and a Proposed Binding Site on Tubulin
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Structural basis for the interaction of antibiotics with the peptidyl transferase centre in eubacteria
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The Mechanism of Action of Macrolides, Lincosamides and Streptogramin B Reveals the Nascent Peptide Exit Path in the Ribosome
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Bioactive marine metabolites. 33. Cyclotheonamides, potent thrombin inhibitors, from a marine sponge Theonella sp
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Amphotericin B Covalent Dimers Forming Sterol-Dependent Ion-Permeable Membrane Channels
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The design, computer modeling, solution structure, and biological evaluation of synthetic analogs of bryostatin 1
resolves10.1021/ja00021a034
Synthesis and analysis of 506BD, a high-affinity ligand for the immunophilin FKBP
resolves10.1016/j.chembiol.2005.10.017
Rapamycin Analogs with Differential Binding Specificity Permit Orthogonal Control of Protein Activity
resolves10.7164/antibiotics.49.230
Antascomicins A, B, C, D and E. Novel FKBP12 Binding Compounds from a Micromonospora Strain.
resolves10.1021/ja963566p
Simultaneous Recognition of a Carboxylate-Containing Ligand and an Intramolecular Surrogate Ligand in the Crystal Structure of an Asymmetric Vancomycin Dimer
resolves10.1002/1521-3765(20010903)7:17<3798::AID-CHEM3798>3.0.CO;2-6
Solid- and Solution-Phase Synthesis of Vancomycin and Vancomycin Analogues with Activity against Vancomycin-Resistant Bacteria
resolves10.1002/1521-3765(20010903)7:17<3824::AID-CHEM3824>3.0.CO;2-1
Synthesis and Biological Evaluation of Vancomycin Dimers with Potent Activity against Vancomycin-Resistant Bacteria: Target-Accelerated Combinatorial Synthesis
resolves10.1111/j.1574-6976.2003.tb00628.x
Mechanism of action of oritavancin and related glycopeptide antibiotics
resolves10.1128/AAC.50.3.899-909.2006
Preclinical Profile of VX-950, a Potent, Selective, and Orally Bioavailable Inhibitor of Hepatitis C Virus NS3-4A Serine Protease
resolves10.1002/anie.200390347
Macrocyclic Inhibitors of the NS3 Protease as Potential Therapeutic Agents of Hepatitis C Virus Infection
resolves10.1021/jm0342414
Structure−Activity Study on a Novel Series of Macrocyclic Inhibitors of the Hepatitis C Virus NS3 Protease Leading to the Discovery of BILN 2061
resolves10.1038/nature02099
An NS3 protease inhibitor with antiviral effects in humans infected with hepatitis C virus
resolves10.1021/ja048170p
Relationship of Stereochemical and Skeletal Diversity of Small Molecules to Cellular Measurement Space
resolves10.1021/jm950588y
(<i>S</i>)-13-[(Dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16,21-dimetheno- 1<i>H</i>,13<i>H</i>-dibenzo[<i>e</i>,<i>k</i>]pyrrolo[3,4-<i>h</i>][1,4,13]oxadiazacyclohexadecene-1,3(2<i>H</i>)-dione (LY333531) and Related Analogues: Isozyme Selective Inhibitors of Protein Kinase Cβ
resolves10.1021/ja050576u
Comparison of the ATP Binding Sites of Protein Kinases Using Conformationally Diverse Bisindolylmaleimides
resolves10.1021/ja0563455
Testing the Conformational Hypothesis of Passive Membrane Permeability Using Synthetic Cyclic Peptide Diastereomers
resolves10.1021/ja063076p
Conformational Flexibility, Internal Hydrogen Bonding, and Passive Membrane Permeability: Successful in Silico Prediction of the Relative Permeabilities of Cyclic Peptides
resolves10.1021/jm060884i
Macrocyclic Inhibitors of β-Secretase: Functional Activity in an Animal Model
resolves10.1021/jm050820s
Novel Potent Hepatitis C Virus NS3 Serine Protease Inhibitors Derived from Proline-Based Macrocycles
resolves10.1021/jm010531d
3-Aminopyrrolidinone Farnesyltransferase Inhibitors: Design of Macrocyclic Compounds with Improved Pharmacokinetics and Excellent Cell Potency
resolves10.1021/ja0256461
Conformationally Constrained Macrocycles That Mimic Tripeptide β-Strands in Water and Aprotic Solvents
resolves10.1021/ja00087a007
Template-Constrained Cyclic Peptides: Design of High-Affinity Ligands for GPIIb/IIIa
resolves10.1007/b96883
Strategies for Total and Diversity-Oriented Synthesis of Natural Product(-Like) Macrocycles
resolves10.1002/anie.200600641
Macrocyclization by Ring‐Closing Metathesis in the Total Synthesis of Natural Products: Reaction Conditions and Limitations
resolves10.1007/s11030-005-1313-y
Macrocycles rapidly produced by multiple multicomponent reactions including bifunctional building blocks (MiBs)
resolves10.1021/ol034907o
Difficult Macrocyclizations: New Strategies for Synthesizing Highly Strained Cyclic Tetrapeptides
resolves10.1002/anie.200351930
Intramolecular Staudinger Ligation: A Powerful Ring‐Closure Method To Form Medium‐Sized Lactams
resolves10.1021/cc020076m
Macrolactones in Diversity-Oriented Synthesis: Preparation of a Pilot Library and Exploration of Factors Controlling Macrocyclization
resolves10.1021/jm0606600
Discovery of a New Class of Macrocyclic Antagonists to the Human Motilin Receptor
resolves10.1126/science.1102629
DNA-Templated Organic Synthesis and Selection of a Library of Macrocycles
resolves10.7164/antibiotics.40.1249
FK-506, a novel immunosuppressant isolated from a Streptomyces. I. Fermentation, isolation, and physico-chemical and biological characteristics.
resolves10.1099/ijs.0.02941-0
Phylogenetic analysis of the genera Streptomyces and Kitasatospora based on partial RNA polymerase β-subunit gene (rpoB) sequences
resolves10.1007/BF02171740
Structural studies on FK-506, cyclosporin A and their immunophilin complexes
resolves10.1021/ja003673q
Conformational Restriction of Flexible Ligands Guided by the Transferred NOE Experiment: Potent Macrocyclic Inhibitors of Farnesyltransferase
resolves10.1021/jm061247v
Structure-Based Design, Synthesis, and Biological Evaluation of Potent and Selective Macrocyclic Checkpoint Kinase 1 Inhibitors
resolves10.1016/j.bbrc.2003.09.029
A novel macrocyclic tetrapeptide mimetic that exhibits low-picomolar Grb2 SH2 domain-binding affinity
resolves10.1016/S0960-894X(02)00527-9
Development of a Phosphatase-Stable Phosphotyrosyl Mimetic Suitably Protected for the Synthesis of High-Affinity Grb2 SH2 Domain-Binding Ligands
resolves10.1016/j.bmcl.2007.02.059
Novel bis(indolyl)maleimide pyridinophanes that are potent, selective inhibitors of glycogen synthase kinase-3
resolves10.1016/j.bmcl.2006.07.026
Structure-based drug design of a highly potent CDK1,2,4,6 inhibitor with novel macrocyclic quinoxalin-2-one structure
resolves10.1002/cmdc.200600199
Macrocyclic Aminopyrimidines as Multitarget CDK and VEGF‐R Inhibitors with Potent Antiproliferative Activities
resolves10.1021/ja0721521
Exploiting Ligand Conformation in Selective Inhibition of Non-Ribosomal Peptide Synthetase Amino Acid Adenylation with Designed Macrocyclic Small Molecules
resolves10.1021/jm049592c
Macrocyclic Inhibitors for Peptide Deformylase: A Structure−Activity Relationship Study of the Ring Size
resolves10.1021/jm00107a004
Renin inhibitors containing conformationally restricted P1-P1' dipeptide mimetics
resolves10.1016/S0040-4039(00)61590-3
Macrocyclic renin inhibitors: Synthesis of a subnanomolar, orally active cysteine derived inhibitor
resolves10.1021/jm000013n
Synthesis, Stability, Antiviral Activity, and Protease-Bound Structures of Substrate-Mimicking Constrained Macrocyclic Inhibitors of HIV-1 Protease
resolves10.1021/jm030337m
Countering Cooperative Effects in Protease Inhibitors Using Constrained β-Strand-Mimicking Templates in Focused Combinatorial Libraries
resolves10.1016/S0960-894X(00)80074-8
Design, synthesis, and activity of conformationally-constrained macrocyclic peptide-based inhibitors of HIV protease
resolves10.1016/0960-894X(96)00034-0
Synthesis and activity of conformationally-constrained macrocyclic norstatine-based inhibitors of HIV protease
resolves10.1021/jm00048a004
Design, Synthesis, and Conformational Analysis of a Novel Macrocyclic HIV-Protease Inhibitor
resolves10.1016/j.bmcl.2007.05.043
Potent macrocyclic antagonists to the motilin receptor presenting novel unnatural amino acids
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no DOI — not checkedSeiwert, S. et al. Preclinical characteristics of ITMN-191, an orally active inhibitor of the HCV NS3/4A protease nominated for preclinical development. Digestive Disease Week 2006, Los Angeles, USA, May 21–24 2006. Array Biopharma web site [ online ], (2006).
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