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Modern Phenotypic Drug Discovery Is a Viable, Neoclassic Pharma Strategy

Journal of medicinal chemistry, 2012-05, Vol.55 (10), p.4527-4538

2012

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Potent oxindole based human β3 adrenergic receptor agonists

Bioorganic & medicinal chemistry letters, 2007-11, Vol.17 (22), p.6270-6273

2007

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d-Phenylglycinol-derived non-covalent factor Xa inhibitors: Effect of non-peptidic S4 linkage elements on affinity and anticoagulant activity

Bioorganic & medicinal chemistry letters, 2007-11, Vol.17 (21), p.5801-5805

2007

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Potent benzimidazolone based human beta(3)-adrenergic receptor agonists

Bioorganic & medicinal chemistry letters, 2006-11, Vol.16 (21), p.5691-5694

2006

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Enantioselective total synthesis of 9S-dihydroerythronolide A seco acid

Journal of the American Chemical Society, 1989-08, Vol.111 (16), p.6247-6256

1989

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1,2-disubstituted indole, azaindole and benzimidazole derivatives possessing amine moiety: a novel series of thrombin inhibitors

Bioorganic & medicinal chemistry letters, 2000-10, Vol.10 (20), p.2347-2351

2000

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Synthesis and evaluation of 3-substituted analogs of 1,2,3,4-tetrahydroisoquinoline as inhibitors of phenylethanolamine N-methyltransferase

Journal of medicinal chemistry, 1988-04, Vol.31 (4), p.824-830

1988

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Inhibition of phenylethanolamine N-methyltransferase (PNMT) by aromatic hydroxy-substituted 1,2,3,4-tetrahydroisoquinolines. Further studies on the hydrophilic pocket of the aromatic ring binding region of the active site

Journal of medicinal chemistry, 1987-12, Vol.30 (12), p.2208-2216

1987

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Abstract 5245: Identification and characterization of the IDO1 inhibitor LY3381916

Cancer research (Chicago, Ill.), 2018-07, Vol.78 (13_Supplement), p.5245-5245

2018

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Fibrinogen Receptor (GPIIb-IIIa) Antagonists Derived from 5,6-Bicyclic Templates. Amidinoindoles, Amidinoindazoles, and Amidinobenzofurans Containing the N-α-Sulfonamide Carboxylic Acid Function as Potent Platelet Aggregation Inhibitors

Journal of medicinal chemistry, 1997-12, Vol.40 (26), p.4308-4318

1997

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Use of Conformationally Restricted Benzamidines as Arginine Surrogates in the Design of Platelet GPIIb-IIIa Receptor Antagonists

Journal of medicinal chemistry, 1997-08, Vol.40 (18), p.2843-2857

1997

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Dibasic benzo[ b]thiophene derivatives as a novel class of active site directed thrombin inhibitors. 2. Exploring interactions at the proximal (S 2) binding site

Bioorganic & medicinal chemistry letters, 1998-09, Vol.8 (18), p.2527-2532

1998

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Conformationally defined adrenergic agents. 13. Conformational and steric aspects of the inhibition of phenylethanolamine N-methyltransferase by benzylamines

Journal of medicinal chemistry, 1988-02, Vol.31 (2), p.433-444

1988

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Abstract 2819: Identification and characterization of a novel smoothened antagonist for the treatment of cancer with deregulated hedgehog signaling

Cancer research (Chicago, Ill.), 2011-04, Vol.71 (8_Supplement), p.2819-2819

2011

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Characterization of the interaction between human .alpha.-thrombin and methyl 3-(2-methyl-1-oxopropoxy) [1]benzothieno[3,2-b]furan-2-carboxylate (LY806303) using electrospray mass spectrometry and tandem mass spectrometry

Journal of medicinal chemistry, 1993-08, Vol.36 (16), p.2350-2355

1993

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Potent oxindole based human beta sub(3) adrenergic receptor agonists

Bioorganic & medicinal chemistry, 2007-11, Vol.17 (22), p.6270-6273

2007

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Potent oxindole based human beta3 adrenergic receptor agonists

Bioorganic & medicinal chemistry letters, 2007-11, Vol.17 (22), p.6270-6273

2007

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Dibasic benzo[ b]thiophene derivatives as a novel class of active site directed thrombin inhibitors: 4. SAR studies on the conformationally restricted C3-side chain of hydroxybenzo[ b]thiophenes

Bioorganic & medicinal chemistry letters, 1999-03, Vol.9 (5), p.759-764

1999

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Potent benzimidazolone based human β3-adrenergic receptor agonists

Bioorganic & medicinal chemistry letters, 2006-11, Vol.16 (21), p.5691-5694

2006

Volltextzugriff (PDF)

Potent oxindole based human β 3 adrenergic receptor agonists

Bioorganic & medicinal chemistry letters, 2007, Vol.17 (22), p.6270-6273

2007

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Conformationally defined adrenergic agents. 10. Binding orientation of amphetamine and norfenfluramine analogs in the benzonorbornene and benzobicyclo[3.2.1]octane ring systems at the active site of phenylethanolamine N-methyltransferase (PNMT)

Journal of medicinal chemistry, 1987-12, Vol.30 (12), p.2191-2208

1987

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Potent benzimidazolone based human beta sub(3)-adrenergic receptor agonists

Bioorganic & medicinal chemistry letters, 2006-11, Vol.16 (21), p.5691-5694

2006

Volltextzugriff (PDF)

Conformationally defined adrenergic agents. 9. Binding requirements of phenolic phenylethylamines in the benzonorbornene skeleton at the active site of phenylethanolamine N-methyltransferase

Journal of medicinal chemistry, 1986-10, Vol.29 (10), p.1972-1982

1986

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Modern Phenotypic Drug Discovery Is a Viable, Neoclassic Pharma Strategy

Potent oxindole based human β3 adrenergic receptor agonists

d-Phenylglycinol-derived non-covalent factor Xa inhibitors: Effect of non-peptidic S4 linkage elements on affinity and anticoagulant activity

Potent benzimidazolone based human beta(3)-adrenergic receptor agonists

Enantioselective total synthesis of 9S-dihydroerythronolide A seco acid

1,2-disubstituted indole, azaindole and benzimidazole derivatives possessing amine moiety: a novel series of thrombin inhibitors

Synthesis and evaluation of 3-substituted analogs of 1,2,3,4-tetrahydroisoquinoline as inhibitors of phenylethanolamine N-methyltransferase

Diamino Benzo[b]thiophene Derivatives as a Novel Class of Active Site Directed Thrombin Inhibitors. 5. Potency, Efficacy, and Pharmacokinetic Properties of Modified C-3 Side Chain Derivatives

Inhibition of phenylethanolamine N-methyltransferase (PNMT) by aromatic hydroxy-substituted 1,2,3,4-tetrahydroisoquinolines. Further studies on the hydrophilic pocket of the aromatic ring binding region of the active site

Abstract 5245: Identification and characterization of the IDO1 inhibitor LY3381916

Fibrinogen Receptor (GPIIb-IIIa) Antagonists Derived from 5,6-Bicyclic Templates. Amidinoindoles, Amidinoindazoles, and Amidinobenzofurans Containing the N-α-Sulfonamide Carboxylic Acid Function as Potent Platelet Aggregation Inhibitors

Use of Conformationally Restricted Benzamidines as Arginine Surrogates in the Design of Platelet GPIIb-IIIa Receptor Antagonists

Dibasic benzo[ b]thiophene derivatives as a novel class of active site directed thrombin inhibitors. 2. Exploring interactions at the proximal (S 2) binding site

Conformationally defined adrenergic agents. 13. Conformational and steric aspects of the inhibition of phenylethanolamine N-methyltransferase by benzylamines

Abstract 2819: Identification and characterization of a novel smoothened antagonist for the treatment of cancer with deregulated hedgehog signaling

Characterization of the interaction between human .alpha.-thrombin and methyl 3-(2-methyl-1-oxopropoxy) [1]benzothieno[3,2-b]furan-2-carboxylate (LY806303) using electrospray mass spectrometry and tandem mass spectrometry

Potent oxindole based human beta sub(3) adrenergic receptor agonists

Potent oxindole based human beta3 adrenergic receptor agonists

Dibasic benzo[ b]thiophene derivatives as a novel class of active site directed thrombin inhibitors: 4. SAR studies on the conformationally restricted C3-side chain of hydroxybenzo[ b]thiophenes

Potent benzimidazolone based human β3-adrenergic receptor agonists

Potent oxindole based human β 3 adrenergic receptor agonists

Conformationally defined adrenergic agents. 10. Binding orientation of amphetamine and norfenfluramine analogs in the benzonorbornene and benzobicyclo[3.2.1]octane ring systems at the active site of phenylethanolamine N-methyltransferase (PNMT)

Dibasic Benzo[b]thiophene Derivatives as a Novel Class of Active Site-Directed Thrombin Inhibitors. 1. Determination of the Serine Protease Selectivity, Structure−Activity Relationships, and Binding Orientation

Potent benzimidazolone based human beta sub(3)-adrenergic receptor agonists

Conformationally defined adrenergic agents. 9. Binding requirements of phenolic phenylethylamines in the benzonorbornene skeleton at the active site of phenylethanolamine N-methyltransferase

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