(Q30952782)

27 June 2017

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title

Lead compounds discovered from libraries: part 2. (English)

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27 June 2017

1

Adam Golebiowski

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27 June 2017

Sean R Klopfenstein

2

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27 June 2017

David E Portlock

series ordinal

3

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27 June 2017

publication date

1 June 2003

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Current Opinion in Chemical Biology

27 June 2017

published in

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27 June 2017

volume

7

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27 June 2017

issue

3

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27 June 2017

page(s)

308-325

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Lead compounds discovered from libraries

27 June 2017

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From protein domains to drug candidates-natural products as guiding principles in the design and synthesis of compound libraries

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7 January 2021

Drugs, leads, and drug-likeness: an analysis of some recently launched drugs

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7 January 2021

Drug discovery: a historical perspective

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7 January 2021

Discovery and parallel synthesis of a new class of cathepsin K inhibitors

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7 January 2021

4-Hydroxy-5,6-dihydropyrones as inhibitors of HIV protease: the effect of heterocyclic substituents at C-6 on antiviral potency and pharmacokinetic parameters

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7 January 2021

Selective cleavage of D-Ala-D-Lac by small molecules: re-sensitizing resistant bacteria to vancomycin

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7 January 2021

1,4-Disubstituted imidazoles are potential antibacterial agents functioning as inhibitors of enoyl acyl carrier protein reductase (FabI)

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7 January 2021

Structure-Activity studies for a novel series of tricyclic dihydropyrimidines as K(ATP) channel openers (KCOs).

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7 January 2021

Discovery of a series of nonpeptide small molecules that inhibit the binding of insulin-like growth factor (IGF) to IGF-binding proteins

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7 January 2021

New antimitotic agents with activity in multi-drug-resistant cell lines and in vivo efficacy in murine tumor models

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7 January 2021

Identification of a subtype selective human PPARalpha agonist through parallel-array synthesis

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7 January 2021

A selective peroxisome proliferator-activated receptor delta agonist promotes reverse cholesterol transport

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7 January 2021

The discovery of acylated beta-amino acids as potent and orally bioavailable VLA-4 antagonists

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7 January 2021

The discovery of sulfonylated dipeptides as potent VLA-4 antagonists

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7 January 2021

Focused library approach for identification of new N-acylphenylalanines as VCAM/VLA-4 antagonists

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7 January 2021

Discovery and initial structure-activity relationships of trisubstituted ureas as thrombin receptor (PAR-1) antagonists

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7 January 2021

Discovery of a nonpeptidic small molecule antagonist of the human platelet thrombin receptor (PAR-1).

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7 January 2021

Thrombin receptor (PAR-1) antagonists. Solid-phase synthesis of indole-based peptide mimetics by anchoring to a secondary amide

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7 January 2021

The first potent and selective inhibitors of the glycine transporter type 2.

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7 January 2021

Use of parallel-synthesis combinatorial libraries for rapid identification of potent FKBP12 inhibitors

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7 January 2021

Solid-phase synthesis of FKBP12 inhibitors: N-sulfonyl and N-carbamoylprolyl/pipecolyl amides

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7 January 2021

A combinatorial library of indinavir analogues and its in vitro and in vivo studies

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7 January 2021

Combinatorial library of indinavir analogues: replacement for the aminoindanol at P2'.

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7 January 2021

Tricyclic isoxazoles are novel inhibitors of the multidrug resistance protein (MRP1).

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7 January 2021

Structure-activity relationship on the human EP3 prostanoid receptor by use of solid-support chemistry

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https://api.crossref.org/works/10.1016%2FS1367-5931%2803%2900059-0

7 January 2021

Structure-activity relationship of biaryl acylsulfonamide analogues on the human EP(3) prostanoid receptor

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7 January 2021

Development of serine protease inhibitors displaying a multicentered short (<2.3 A) hydrogen bond binding mode: inhibitors of urokinase-type plasminogen activator and factor Xa.

1 reference

https://api.crossref.org/works/10.1016%2FS1367-5931%2803%2900059-0

7 January 2021

4-Aminoarylguanidine and 4-aminobenzamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors

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https://api.crossref.org/works/10.1016%2FS1367-5931%2803%2900059-0

7 January 2021

1-[2-[(5-Cyanopyridin-2-yl)amino]ethylamino]acetyl-2-(S)-pyrrolidinecarbonitrile: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties

1 reference

https://api.crossref.org/works/10.1016%2FS1367-5931%2803%2900059-0

7 January 2021

Discovery of further pyrrolidine trans-lactams as inhibitors of human neutrophil elastase (HNE) with potential as development candidates and the crystal structure of HNE complexed with an inhibitor (GW475151)

1 reference

https://api.crossref.org/works/10.1016%2FS1367-5931%2803%2900059-0

7 January 2021

Click chemistry in situ: acetylcholinesterase as a reaction vessel for the selective assembly of a femtomolar inhibitor from an array of building blocks

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https://api.crossref.org/works/10.1016%2FS1367-5931%2803%2900059-0

7 January 2021

Small-molecule antagonists of Myc/Max dimerization inhibit Myc-induced transformation of chicken embryo fibroblasts

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https://api.crossref.org/works/10.1016%2FS1367-5931%2803%2900059-0

7 January 2021

Erythropoietin mimetics derived from solution phase combinatorial libraries

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https://api.crossref.org/works/10.1016%2FS1367-5931%2803%2900059-0

7 January 2021

Design, synthesis, and evaluation of opioid analogues with non-peptidic beta-turn scaffold: enkephalin and endomorphin mimetics

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https://api.crossref.org/works/10.1016%2FS1367-5931%2803%2900059-0

7 January 2021

The identification and characterization of hydrazinyl urea-based antibacterial agents through combinatorial chemistry

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https://api.crossref.org/works/10.1016%2FS1367-5931%2803%2900059-0

7 January 2021

Synthesis and structure-activity relationship study of potent trypanocidal thio semicarbazone inhibitors of the trypanosomal cysteine protease cruzain

1 reference

https://api.crossref.org/works/10.1016%2FS1367-5931%2803%2900059-0

7 January 2021

Nanomolar inhibitors of Staphylococcus aureus methionyl tRNA synthetase with potent antibacterial activity against gram-positive pathogens.

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https://api.crossref.org/works/10.1016%2FS1367-5931%2803%2900059-0

7 January 2021

Optimization of a screening lead for factor VIIa/TF.

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7 January 2021

The discovery of small molecule carbamates as potent dual alpha(4)beta(1)/alpha(4)beta(7) integrin antagonists

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7 January 2021

4-Aminoquinolines as a novel class of NR1/2B subtype selective NMDA receptor antagonists

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7 January 2021

Design, synthesis, and structural analysis of influenza neuraminidase inhibitors containing pyrrolidine cores

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7 January 2021

The discovery of RFI-641 as a potent and selective inhibitor of the respiratory syncytial virus

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7 January 2021

Protein kinases--the major drug targets of the twenty-first century?

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https://api.crossref.org/works/10.1016%2FS1367-5931%2803%2900059-0

7 January 2021

Discovery of a new class of p38 kinase inhibitors

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https://api.crossref.org/works/10.1016%2FS1367-5931%2803%2900059-0

7 January 2021

Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site

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https://api.crossref.org/works/10.1016%2FS1367-5931%2803%2900059-0

7 January 2021

Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate

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https://api.crossref.org/works/10.1016%2FS1367-5931%2803%2900059-0

7 January 2021

p38 kinase inhibitors for the treatment of arthritis and osteoporosis: thienyl, furyl, and pyrrolyl ureas

1 reference

https://api.crossref.org/works/10.1016%2FS1367-5931%2803%2900059-0

7 January 2021

Synthesis and pharmacological characterization of a potent, orally active p38 kinase inhibitor

1 reference

https://api.crossref.org/works/10.1016%2FS1367-5931%2803%2900059-0

7 January 2021

Discovery of heterocyclic ureas as a new class of raf kinase inhibitors: identification of a second generation lead by a combinatorial chemistry approach

1 reference

https://api.crossref.org/works/10.1016%2FS1367-5931%2803%2900059-0

7 January 2021

Discovery of a novel Raf kinase inhibitor

1 reference

https://api.crossref.org/works/10.1016%2FS1367-5931%2803%2900059-0

7 January 2021

The discovery of RPR 200765A, a p38 MAP kinase inhibitor displaying a good oral anti-arthritic efficacy

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https://api.crossref.org/works/10.1016%2FS1367-5931%2803%2900059-0

7 January 2021

An algorithm-directed two-component library synthesized via solid-phase methodology yielding potent and orally bioavailable p38 MAP kinase inhibitors

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https://api.crossref.org/works/10.1016%2FS1367-5931%2803%2900059-0

7 January 2021

Phenoxypyrimidine inhibitors of p38alpha kinase: synthesis and statistical evaluation of the p38 inhibitory potencies of a series of 1-(piperidin-4-yl)-4-(4-fluorophenyl)-5-(2-phenoxypyrimidin-4-yl) imidazoles

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7 January 2021

Synthesis and initial SAR studies of 3,6-disubstituted pyrazolo[1,5-a]pyrimidines: a new class of KDR kinase inhibitors

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https://api.crossref.org/works/10.1016%2FS1367-5931%2803%2900059-0

7 January 2021

Discovery and initial SAR of imidazoquinoxalines as inhibitors of the Src-family kinase p56(Lck).

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https://api.crossref.org/works/10.1016%2FS1367-5931%2803%2900059-0

7 January 2021

Structure-activity studies of 5-substituted pyridopyrimidines as adenosine kinase inhibitors

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https://api.crossref.org/works/10.1016%2FS1367-5931%2803%2900059-0

7 January 2021

Pyridopyrimidine analogues as novel adenosine kinase inhibitors

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7 January 2021

Identification of novel inhibitors of the transforming growth factor beta1 (TGF-beta1) type 1 receptor (ALK5).

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7 January 2021

Synthesis and bioactivities of novel 4,5,6,7-tetrahydrothieno[2,3-c]pyridines as inhibitors of tumor necrosis factor-alpha (TNF-alpha) production

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https://api.crossref.org/works/10.1016%2FS1367-5931%2803%2900059-0

7 January 2021

Synthesis and PTP1B inhibition of 1,2-naphthoquinone derivatives as potent anti-diabetic agents

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7 January 2021

Discovery of aminothiazole inhibitors of cyclin-dependent kinase 2: synthesis, X-ray crystallographic analysis, and biological activities

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https://api.crossref.org/works/10.1016%2FS1367-5931%2803%2900059-0

7 January 2021

3-Anilino-4-arylmaleimides: potent and selective inhibitors of glycogen synthase kinase-3 (GSK-3).

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https://api.crossref.org/works/10.1016%2FS1367-5931%2803%2900059-0

7 January 2021

Substituted imidazoles as glucagon receptor antagonists

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https://api.crossref.org/works/10.1016%2FS1367-5931%2803%2900059-0

7 January 2021

Identification of alkylidene hydrazides as glucagon receptor antagonists.

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https://api.crossref.org/works/10.1016%2FS1367-5931%2803%2900059-0

7 January 2021

Discovery of 5-hydroxyalkyl-4-phenylpyridines as a new class of glucagon receptor antagonists

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7 January 2021

Optimization of the 4-aryl group of 4-aryl-pyridine glucagon antagonists: development of an efficient, alternative synthesis

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7 January 2021

Beta 3 agonists. Part 1: evolution from inception to BMS-194449.

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7 January 2021

BMS-196085: a potent and selective full agonist of the human beta(3) adrenergic receptor

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7 January 2021

2-(Anilinomethyl)imidazolines as alpha1 adrenergic receptor agonists: the discovery of alpha1a subtype selective 2'-alkylsulfonyl-substituted analogues

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7 January 2021

CCR3 antagonists: a potential new therapy for the treatment of asthma. Discovery and structure-activity relationships

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7 January 2021

Discovery and structure-activity relationship of N-(ureidoalkyl)-benzyl-piperidines as potent small molecule CC chemokine receptor-3 (CCR3) antagonists.

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7 January 2021

Piperazine-based CCR5 antagonists as HIV-1 inhibitors. I: 2(S)-methyl piperazine as a key pharmacophore element

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https://api.crossref.org/works/10.1016%2FS1367-5931%2803%2900059-0

7 January 2021

Discovery of 4-[(Z)-(4-bromophenyl)- (ethoxyimino)methyl]-1'-[(2,4-dimethyl-3- pyridinyl)carbonyl]-4'-methyl-1,4'- bipiperidine N-oxide (SCH 351125): an orally bioavailable human CCR5 antagonist for the treatment of HIV infection

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7 January 2021

Synthesis, SAR, and biological evaluation of oximino-piperidino-piperidine amides. 1. Orally bioavailable CCR5 receptor antagonists with potent anti-HIV activity

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https://api.crossref.org/works/10.1016%2FS1367-5931%2803%2900059-0

7 January 2021

Antagonists of the human CCR5 receptor as anti-HIV-1 agents. part 1: discovery and initial structure-activity relationships for 1 -amino-2-phenyl-4-(piperidin-1-yl)butanes

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https://api.crossref.org/works/10.1016%2FS1367-5931%2803%2900059-0

7 January 2021

Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 2: structure-activity relationships for substituted 2-Aryl-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-(piperidin-1-yl)butanes

1 reference

https://api.crossref.org/works/10.1016%2FS1367-5931%2803%2900059-0

7 January 2021

1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 1: discovery of the pyrrolidine scaffold and determination of its stereochemical requirements

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https://api.crossref.org/works/10.1016%2FS1367-5931%2803%2900059-0

7 January 2021

1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 2: lead optimization affording selective, orally bioavailable compounds with potent anti-HIV activity

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https://api.crossref.org/works/10.1016%2FS1367-5931%2803%2900059-0

7 January 2021

Combinatorial synthesis of CCR5 antagonists

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7 January 2021

Initial structure-activity relationship of a novel class of nonpeptidyl GnRH receptor antagonists: 2-arylindoles

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7 January 2021

SAR studies of novel 5-substituted 2-arylindoles as nonpeptidyl GnRH receptor antagonists

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7 January 2021

Substituted indole-5-carboxamides and -acetamides as potent nonpeptide GnRH receptor antagonists

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7 January 2021

Potent nonpeptide GnRH receptor antagonists derived from substituted indole-5-carboxamides and -acetamides bearing a pyridine side-chain terminus

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https://api.crossref.org/works/10.1016%2FS1367-5931%2803%2900059-0

7 January 2021

Orally bioavailable, indole-based nonpeptide GnRH receptor antagonists with high potency and functional activity

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7 January 2021

A potent, nonpeptidyl 1H-quinolone antagonist for the gonadotropin-releasing hormone receptor

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7 January 2021

Combinatorial synthesis of 3-(amidoalkyl) and 3-(aminoalkyl)-2-arylindole derivatives: discovery of potent ligands for a variety of G-protein coupled receptors

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7 January 2021

2-Aryl indole NK1 receptor antagonists: optimisation of indole substitution

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7 January 2021

2-Aryl indole NK1 receptor antagonists: optimisation of the 2-aryl ring and the indole nitrogen substituent

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7 January 2021

2-Aryl indole NK(1) antagonists: optimisation of the amide substituent

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7 January 2021

Expedited discovery of second generation NK-1 antagonists: identification of a nonbasic aryloxy substituent

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https://api.crossref.org/works/10.1016%2FS1367-5931%2803%2900059-0

7 January 2021

Dihydropyridine neuropeptide Y Y(1) receptor antagonists

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https://api.crossref.org/works/10.1016%2FS1367-5931%2803%2900059-0

7 January 2021

Aminopyrazoles with high affinity for the human neuropeptide Y5 receptor

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https://api.crossref.org/works/10.1016%2FS1367-5931%2803%2900059-0

7 January 2021

Pyrazolecarboxamide human neuropeptide Y5 receptor ligands with in vivo antifeedant activity

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7 January 2021

Novel potent antagonists of human neuropeptide Y Y5 receptor. Part 1: 2-oxobenzothiazolin-3-acetic acid derivatives

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https://api.crossref.org/works/10.1016%2FS1367-5931%2803%2900059-0

7 January 2021

Novel potent antagonists of human neuropeptide Y-Y5 receptor. Part 4: tetrahydrodiazabenzazulene derivatives

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https://api.crossref.org/works/10.1016%2FS1367-5931%2803%2900059-0

7 January 2021

Synthesis and structure-activity relationships of trisubstituted phenyl urea derivatives as neuropeptide Y5 receptor antagonists

1 reference

https://api.crossref.org/works/10.1016%2FS1367-5931%2803%2900059-0

7 January 2021

High-throughput synthesis optimization of sulfonamide NPY Y5 antagonists

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https://api.crossref.org/works/10.1016%2FS1367-5931%2803%2900059-0

7 January 2021

Targeting signal transduction with large combinatorial collections

1 reference

https://api.crossref.org/works/10.1016%2FS1367-5931%2803%2900059-0

7 January 2021

10.1016/S1367-5931(03)00059-0

Identifiers

DOI

1 reference

27 June 2017

1 reference