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The Medicinal Chemistry of Therapeutic Oligonucleotides

Journal of medicinal chemistry, 2016-11, Vol.59 (21), p.9645-9667

2016

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Towards next generation antisense oligonucleotides: mesylphosphoramidate modification improves therapeutic index and duration of effect of gapmer antisense oligonucleotides

Nucleic acids research, 2021-09, Vol.49 (16), p.9026-9041

2021

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Site-specific replacement of phosphorothioate with alkyl phosphonate linkages enhances the therapeutic profile of gapmer ASOs by modulating interactions with cellular proteins

Nucleic acids research, 2019-06, Vol.47 (11), p.5465-5479

2019

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Understanding the effect of controlling phosphorothioate chirality in the DNA gap on the potency and safety of gapmer antisense oligonucleotides

Nucleic acids research, 2020-02, Vol.48 (4), p.1691-1700

2020

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Simultaneous inhibition of endocytic recycling and lysosomal fusion sensitizes cells and tissues to oligonucleotide therapeutics

Nucleic acids research, 2023-02, Vol.51 (4), p.1583-1599

2023

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Synthesis, biophysical properties and biological activity of second generation antisense oligonucleotides containing chiral phosphorothioate linkages

Nucleic acids research, 2014-12, Vol.42 (22), p.13456-13468

2014

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Site-specific incorporation of 5'-methyl DNA enhances the therapeutic profile of gapmer ASOs

Nucleic acids research, 2021-02, Vol.49 (4), p.1828-1839

2021

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Comprehensive Structure–Activity Relationship of Triantennary N‑Acetylgalactosamine Conjugated Antisense Oligonucleotides for Targeted Delivery to Hepatocytes

Journal of medicinal chemistry, 2016-03, Vol.59 (6), p.2718-2733

2016

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Efficient Synthesis and Biological Evaluation of 5′-GalNAc Conjugated Antisense Oligonucleotides

Bioconjugate chemistry, 2015-08, Vol.26 (8), p.1451-1455

2015

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Evaluation of Phosphorus and Non-Phosphorus Neutral Oligonucleotide Backbones for Enhancing Therapeutic Index of Gapmer Antisense Oligonucleotides

Nucleic acid therapeutics, 2022-02, Vol.32 (1), p.40-50

2022

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Solid-phase synthesis of 5′-triantennary N-acetylgalactosamine conjugated antisense oligonucleotides using phosphoramidite chemistry

Bioorganic & medicinal chemistry letters, 2015-10, Vol.25 (19), p.4127-4130

2015

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Effect of diastereoisomeric composition on the chromatographic retention of phosphorothioated oligonucleotides using three different liquid chromatography systems

Journal of Chromatography A, 2024-08, Vol.1730, p.465108, Article 465108

2024

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A convenient synthesis of 5′-triantennary N-acetyl-galactosamine clusters based on nitromethanetrispropionic acid

Bioorganic & medicinal chemistry letters, 2016-05, Vol.26 (9), p.2194-2197

2016

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Oral Treatment of Cowpox and Vaccinia Virus Infections in Mice with Ether Lipid Esters of Cidofovir

Antimicrobial Agents and Chemotherapy, 2004-02, Vol.48 (2), p.404-412

2004

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Comparative Activities of Lipid Esters of Cidofovir and Cyclic Cidofovir against Replication of Herpesviruses In Vitro

Antimicrobial Agents and Chemotherapy, 2005-09, Vol.49 (9), p.3724-3733

2005

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Oral Activity of Ether Lipid Ester Prodrugs of Cidofovir against Experimental Human Cytomegalovirus Infection

The Journal of infectious diseases, 2004-08, Vol.190 (3), p.499-503

2004

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Oral Treatment of Murine Cytomegalovirus Infections with Ether Lipid Esters of Cidofovir

Antimicrobial Agents and Chemotherapy, 2004-09, Vol.48 (9), p.3516-3522

2004

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Endosomal Escape of Antisense Oligonucleotides Internalized by Stabilin Receptors Is Regulated by Rab5C and EEA1 During Endosomal Maturation

Nucleic acid therapeutics, 2018-04, Vol.28 (2), p.86-96

2018

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Effect of oral treatment with ( S)-HPMPA, HDP-( S)-HPMPA or ODE-( S)-HPMPA on replication of murine cytomegalovirus (MCMV) or human cytomegalovirus (HCMV) in animal models

Antiviral research, 2008-08, Vol.79 (2), p.133-135

2008

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Esterification of cidofovir with alkoxyalkanols increases oral bioavailability and diminishes drug accumulation in kidney

Antiviral research, 2003-08, Vol.59 (3), p.163-171

2003

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Carbon Networks Based on Dehydrobenzoannulenes. 4. Synthesis of “Star” and “Trefoil” Graphdiyne Substructures via Sixfold Cross-Coupling of Hexaiodobenzene

Journal of organic chemistry, 2001-06, Vol.66 (11), p.3893-3901

2001

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Synthesis of Expanded Graphdiyne Substructures

Chemistry : a European journal, 2000-06, Vol.6 (11), p.2044-2052

2000

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Synthesis and Spectroscopic Studies of Expanded Planar Dehydrotribenzo[n]annulenes Containing One or Two Isolated Alkene Units

European journal of organic chemistry, 2001-09, Vol.2001 (18), p.3485-3490

2001

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A versatile synthetic route to dehydrobenzoannulenes via in situ generation of reactive alkynes

Tetrahedron, 2001-04, Vol.57 (17), p.3507-3520

2001

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One-Pot Desilylation/Dimerization of Ethynyl- and Butadiynyltrimethylsilanes. Synthesis of Tetrayne-Linked Dehydrobenzoannulenes

Tetrahedron letters, 1997-10, Vol.38 (43), p.7483-7486

1997

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The Medicinal Chemistry of Therapeutic Oligonucleotides

Towards next generation antisense oligonucleotides: mesylphosphoramidate modification improves therapeutic index and duration of effect of gapmer antisense oligonucleotides

Site-specific replacement of phosphorothioate with alkyl phosphonate linkages enhances the therapeutic profile of gapmer ASOs by modulating interactions with cellular proteins

Understanding the effect of controlling phosphorothioate chirality in the DNA gap on the potency and safety of gapmer antisense oligonucleotides

Simultaneous inhibition of endocytic recycling and lysosomal fusion sensitizes cells and tissues to oligonucleotide therapeutics

Synthesis, biophysical properties and biological activity of second generation antisense oligonucleotides containing chiral phosphorothioate linkages

Site-specific incorporation of 5'-methyl DNA enhances the therapeutic profile of gapmer ASOs

Comprehensive Structure–Activity Relationship of Triantennary N‑Acetylgalactosamine Conjugated Antisense Oligonucleotides for Targeted Delivery to Hepatocytes

Efficient Synthesis and Biological Evaluation of 5′-GalNAc Conjugated Antisense Oligonucleotides

Evaluation of Phosphorus and Non-Phosphorus Neutral Oligonucleotide Backbones for Enhancing Therapeutic Index of Gapmer Antisense Oligonucleotides

Solid-phase synthesis of 5′-triantennary N-acetylgalactosamine conjugated antisense oligonucleotides using phosphoramidite chemistry

Effect of diastereoisomeric composition on the chromatographic retention of phosphorothioated oligonucleotides using three different liquid chromatography systems

A convenient synthesis of 5′-triantennary N-acetyl-galactosamine clusters based on nitromethanetrispropionic acid

Oral Treatment of Cowpox and Vaccinia Virus Infections in Mice with Ether Lipid Esters of Cidofovir

Comparative Activities of Lipid Esters of Cidofovir and Cyclic Cidofovir against Replication of Herpesviruses In Vitro

Oral Activity of Ether Lipid Ester Prodrugs of Cidofovir against Experimental Human Cytomegalovirus Infection

Oral Treatment of Murine Cytomegalovirus Infections with Ether Lipid Esters of Cidofovir

Endosomal Escape of Antisense Oligonucleotides Internalized by Stabilin Receptors Is Regulated by Rab5C and EEA1 During Endosomal Maturation

Effect of oral treatment with ( S)-HPMPA, HDP-( S)-HPMPA or ODE-( S)-HPMPA on replication of murine cytomegalovirus (MCMV) or human cytomegalovirus (HCMV) in animal models

Esterification of cidofovir with alkoxyalkanols increases oral bioavailability and diminishes drug accumulation in kidney

Carbon Networks Based on Dehydrobenzoannulenes. 4. Synthesis of “Star” and “Trefoil” Graphdiyne Substructures via Sixfold Cross-Coupling of Hexaiodobenzene

Synthesis of Expanded Graphdiyne Substructures

Synthesis and Spectroscopic Studies of Expanded Planar Dehydrotribenzo[n]annulenes Containing One or Two Isolated Alkene Units

A versatile synthetic route to dehydrobenzoannulenes via in situ generation of reactive alkynes

One-Pot Desilylation/Dimerization of Ethynyl- and Butadiynyltrimethylsilanes. Synthesis of Tetrayne-Linked Dehydrobenzoannulenes

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