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The importance of synthetic chemistry in the pharmaceutical industry

Science (American Association for the Advancement of Science), 2019-01, Vol.363 (6424)

2019

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The Impact of Chemical Probes in Drug Discovery: A Pharmaceutical Industry Perspective

Cell chemical biology, 2016-01, Vol.23 (1), p.10-17

2016

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Discovery of Pyrophosphate Diesters as Tunable, Soluble, and Bioorthogonal Linkers for Site-Specific Antibody–Drug Conjugates

Journal of the American Chemical Society, 2016-02, Vol.138 (4), p.1430-1445

2016

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Concise Asymmetric Syntheses of Radicicol and Monocillin I

Journal of the American Chemical Society, 2001-11, Vol.123 (44), p.10903-10908

2001

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Discovery of allosteric inhibitors of kinesin spindle protein (KSP) for the treatment of taxane-refractory cancer: MK-0731 and analogs

Anti-cancer agents in medicinal chemistry, 2010-11, Vol.10 (9), p.697-712

2010

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Orally Bioavailable Macrocyclic Peptide That Inhibits Binding of PCSK9 to the Low Density Lipoprotein Receptor

Circulation (New York, N.Y.), 2023-07, Vol.148 (2), p.144-158

2023

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Novel Phosphate Modified Cathepsin B Linkers: Improving Aqueous Solubility and Enhancing Payload Scope of ADCs

Bioconjugate chemistry, 2016-09, Vol.27 (9), p.2081-2088

2016

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3-Aryl-5-phenoxymethyl-1,3-oxazolidin-2-ones as positive allosteric modulators of mGluR2 for the treatment of schizophrenia: Hit-to-lead efforts

Bioorganic & medicinal chemistry letters, 2010-05, Vol.20 (10), p.3129-3133

2010

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CC-1065 and the Duocarmycins: Synthetic Studies

Chemical reviews, 1997-05, Vol.97 (3), p.787-828

1997

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Multiple Synthetic Routes to the Mini-Protein Omomyc and Coiled-Coil Domain Truncations

Journal of organic chemistry, 2020-02, Vol.85 (3), p.1466-1475

2020

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Total Synthesis as a Resource in the Discovery of Potentially Valuable Antitumor Agents: Cycloproparadicicol

Angewandte Chemie International Edition, 2003-03, Vol.42 (11), p.1280-1284

2003

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Discovery of Insulin Receptor Partial Agonists MK-5160 and MK-1092 as Novel Basal Insulins with Potential to Improve Therapeutic Index

Journal of medicinal chemistry, 2022-04, Vol.65 (7), p.5593-5605

2022

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Optimization of a pyrazoloquinolinone class of Chk1 kinase inhibitors

Bioorganic & medicinal chemistry letters, 2007-11, Vol.17 (21), p.5989-5994

2007

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Efficient Asymmetric Synthesis of Radicicol Dimethyl Ether: A Novel Application of Ring-Forming Olefin Metathesis

Organic letters, 2000-10, Vol.2 (20), p.3127-3129

2000

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Regioselective Inverse Electron Demand Diels−Alder Reactions of N-Acyl 6-Amino-3-(methylthio)-1,2,4,5-tetrazines

Journal of organic chemistry, 1998-09, Vol.63 (18), p.6329-6337

1998

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Endosomolytic Bioreducible Poly(amido amine disulfide) Polymer Conjugates for the in Vivo Systemic Delivery of siRNA Therapeutics

Bioconjugate chemistry, 2013-04, Vol.24 (4), p.640-647

2013

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Kinesin spindle protein (KSP) inhibitors. Part 7: Design and synthesis of 3,3-disubstituted dihydropyrazolobenzoxazines as potent inhibitors of the mitotic kinesin KSP

Bioorganic & medicinal chemistry letters, 2007-10, Vol.17 (20), p.5671-5676

2007

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Shape-Dependent Catalysis: Insights into the Source of Catalysis for the CC-1065 and Duocarmycin DNA Alkylation Reaction

Accounts of chemical research, 1999-12, Vol.32 (12), p.1043-1052

1999

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Development of thioquinazolinones, allosteric Chk1 kinase inhibitors

Bioorganic & medicinal chemistry letters, 2009-02, Vol.19 (4), p.1240-1244

2009

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Adenosine analogue inhibitors of S-adenosylhomocysteine hydrolase

Bioorganic & medicinal chemistry letters, 2014-06, Vol.24 (12), p.2737-2740

2014

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Discovery of 5-aryl-1,3-dihydro-2H-imidazo[4,5-b]pyridin-2-ones as positive allosteric modulators of metabotropic glutamate subtype-2 (mGlu2) receptors with efficacy in a preclinical model of psychosis

Bioorganic & medicinal chemistry letters, 2016-02, Vol.26 (4), p.1260-1264

2016

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Improving the In Vivo Therapeutic Index of siRNA Polymer Conjugates through Increasing pH Responsiveness

Bioconjugate chemistry, 2014-02, Vol.25 (2), p.296-307

2014

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An in vivo evaluation of amphiphilic, biodegradable peptide copolymers as siRNA delivery agents

International journal of pharmaceutics, 2014-05, Vol.466 (1-2), p.58-67

2014

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The importance of synthetic chemistry in the pharmaceutical industry

The Impact of Chemical Probes in Drug Discovery: A Pharmaceutical Industry Perspective

Discovery of Pyrophosphate Diesters as Tunable, Soluble, and Bioorthogonal Linkers for Site-Specific Antibody–Drug Conjugates

Concise Asymmetric Syntheses of Radicicol and Monocillin I

Discovery of allosteric inhibitors of kinesin spindle protein (KSP) for the treatment of taxane-refractory cancer: MK-0731 and analogs

Orally Bioavailable Macrocyclic Peptide That Inhibits Binding of PCSK9 to the Low Density Lipoprotein Receptor

Novel Phosphate Modified Cathepsin B Linkers: Improving Aqueous Solubility and Enhancing Payload Scope of ADCs

3-Aryl-5-phenoxymethyl-1,3-oxazolidin-2-ones as positive allosteric modulators of mGluR2 for the treatment of schizophrenia: Hit-to-lead efforts

CC-1065 and the Duocarmycins: Synthetic Studies

Multiple Synthetic Routes to the Mini-Protein Omomyc and Coiled-Coil Domain Truncations

Total Synthesis as a Resource in the Discovery of Potentially Valuable Antitumor Agents: Cycloproparadicicol

Discovery of Insulin Receptor Partial Agonists MK-5160 and MK-1092 as Novel Basal Insulins with Potential to Improve Therapeutic Index

Optimization of a pyrazoloquinolinone class of Chk1 kinase inhibitors

Efficient Asymmetric Synthesis of Radicicol Dimethyl Ether: A Novel Application of Ring-Forming Olefin Metathesis

Kinesin Spindle Protein (KSP) Inhibitors. 9. Discovery of (2S)-4-(2,5-Difluorophenyl)-N-[(3R,4S)-3-fluoro-1-methylpiperidin-4-yl]-2-(hydroxymethyl)-N-methyl-2-phenyl-2,5-dihydro-1H-pyrrole-1-carboxamide (MK-0731) for the Treatment of Taxane-Refractory Cancer

Regioselective Inverse Electron Demand Diels−Alder Reactions of N-Acyl 6-Amino-3-(methylthio)-1,2,4,5-tetrazines

Endosomolytic Bioreducible Poly(amido amine disulfide) Polymer Conjugates for the in Vivo Systemic Delivery of siRNA Therapeutics

Development of a liver-targeted siRNA delivery platform with a broad therapeutic window utilizing biodegradable polypeptide-based polymer conjugates

Kinesin spindle protein (KSP) inhibitors. Part 7: Design and synthesis of 3,3-disubstituted dihydropyrazolobenzoxazines as potent inhibitors of the mitotic kinesin KSP

Shape-Dependent Catalysis: Insights into the Source of Catalysis for the CC-1065 and Duocarmycin DNA Alkylation Reaction

Development of thioquinazolinones, allosteric Chk1 kinase inhibitors

Adenosine analogue inhibitors of S-adenosylhomocysteine hydrolase

Discovery of 5-aryl-1,3-dihydro-2H-imidazo[4,5-b]pyridin-2-ones as positive allosteric modulators of metabotropic glutamate subtype-2 (mGlu2) receptors with efficacy in a preclinical model of psychosis

Improving the In Vivo Therapeutic Index of siRNA Polymer Conjugates through Increasing pH Responsiveness

An in vivo evaluation of amphiphilic, biodegradable peptide copolymers as siRNA delivery agents

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