A. San-Félix

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Double Arylation of the Indole Side Chain of Tri- and Tetrapodal Tryptophan Derivatives Renders Highly Potent HIV-1 and EV-A71 Entry Inhibitors

F. Gago, J. Neyts, D. Schols, 2021, Journal of medicinal chemistry.

TSAO derivatives, inhibitors of HIV-1 reverse transcriptase dimerization: recent progress.

S. de Castro, M. Camarasa, S. Velázquez, 2006, Current pharmaceutical design.

1,2,3-Triazole-[2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D- ribofuranosyl]-3'-spiro-5"-(4"-amino-1",2"-oxathiole 2",2"-dioxide) (TSAO) analogues: synthesis and anti-HIV-1 activity.

E. De Clercq, C. Perno, J. Balzarini, 1994, Journal of medicinal chemistry.

Modifications in the branched arms of a class of dual inhibitors of HIV and EV71 replication expand their antiviral spectrum

L. Delang, J. Neyts, D. Schols, 2019, Antiviral Research.

Targeting HIV entry through interaction with envelope glycoprotein 120 (gp120): synthesis and antiviral evaluation of 1,3,5-triazines with aromatic amino acids.

J. Balzarini, D. Schols, M. Camarasa, 2011, Journal of medicinal chemistry.

Linear and branched alkyl-esters and amides of gallic acid and other (mono-, di- and tri-) hydroxy benzoyl derivatives as promising anti-HCV inhibitors.

J. Neyts, J. Balzarini, M. Camarasa, 2015, European journal of medicinal chemistry.

Identification of L. infantum trypanothione synthetase inhibitors with leishmanicidal activity from a (non-biased) in-house chemical library.

F. Gago, M. Camarasa, S. Velázquez, 2022, European journal of medicinal chemistry.

A Novel Class of Cationic and Non-Peptidic Small Molecules as Hits for the Development of Antimicrobial Agents

M. Camarasa, F. García-del Portillo, M. Pérez-Pérez, 2018, Molecules.

Galloyl Carbohydrates with Antiangiogenic Activity Mediated by Capillary Morphogenesis Gene 2 (CMG2) Protein Binding.

K. Christensen, M. Camarasa, M. S. Rogers, 2019, Journal of medicinal chemistry.

Synthesis of 3-Spiro-Substituted Nucleosides: Chemistry of TSAO Nucleoside Derivatives

M. Camarasa, S. Velázquez, M. Pérez-Pérez, 2013 .

Viral engagement with host receptors blocked by a novel class of tryptophan dendrimers that targets the 5-fold-axis of the enterovirus-A71 capsid

F. Gago, Hyunwook Lee, S. Hafenstein, 2019, PLoS pathogens.

TSAO Derivatives the First Non-Peptide Inhibitors of HIV-1 RT Dimerization

M. Camarasa, S. Velázquez, M. Pérez-Pérez, 2005, Antiviral chemistry & chemotherapy.

The Role of Thr139 in the Human Immunodeficiency Virus Type 1 Reverse Transcriptase Sensitivity to (+)-Calanolide A

E. De Clercq, F. Ceccherini‐Silberstein, F. Gago, 2005, Molecular Pharmacology.

Multivalent agents containing 1-substituted 2,3,4-trihydroxyphenyl moieties as novel synthetic polyphenols directed against HIV-1.

J. Balzarini, M. Camarasa, E. Quesada, 2014, Organic & biomolecular chemistry.

[2',5'-Bis-O-(tert-butyldimethylsilyl)]-3'-spiro-5''-(4''-amino-1'',2''-oxathiole-2'',2''-dioxide) (TSAO) derivatives of purine and pyrimidinenucleosides as potent and selective inhibitors of human immunodeficiency virus type 1

E. De Clercq, J. Balzarini, M. Camarasa, 1992, Antimicrobial Agents and Chemotherapy.

,5 '-Bis-O-(tert-Butyldimethylsilyl)]-3' -Spiro-5"-(4"-Amino-1",2"-Oxathiole-2",2"-Dioxide) (TSAO) Derivatives of Purine and Pyrimidine Nucleosides as Potent and Selective Inhibitors of Human Immunodeficiency Virus Type 1

J. Balzarini, M. Camarasa, S. Velázquez, 2022 .

Synthesis of {1-[2′,5′-Bis-O-(t-butyldimethylsilyl)-β-d-xylo- and β-d-ribofuranosyl]thymine}-3′-spiro-5″-{4″-amino-1″,2″-oxathiole-2″,2″-dioxide} (TSAO). A novel type of specific anti-HIV agents

J. Balzarini, M. Pérez-Pérez, A. San-Félix, 1992 .

Exploring the role of the 5'-position of TSAO-T. Synthesis and anti-HIV evaluation of novel TSAO-T derivatives.

E. De Clercq, F. Gago, J. Balzarini, 2001, Antiviral research.

Structure‐activity relationship studies on a Trp dendrimer with dual activities against HIV and enterovirus A71. Modifications on the amino acid

J. Neyts, J. Balzarini, D. Schols, 2017, Antiviral research.

Selective inhibition of human inmunodeficiency virus type 1 ( HIV-1 ) by nucleoside analogues with an unusual tricyclic structure

J. Balzarini, M. Camarasa, E. Quesada, 2014 .

Selective inhibition of Human Immunodeficiency Virus type 1 (HIV-1) by a novel family of tricyclic nucleosides.

E. Vanstreels, J. Balzarini, M. Camarasa, 2011, Antiviral research.

Synthesis and anti-HIV activity of [AZT]-[TSAO-T] and [AZT]-[HEPT] dimers as potential multifunctional inhibitors of HIV-1 reverse transcriptase.

E. De Clercq, J. Balzarini, M. Camarasa, 1995, Journal of medicinal chemistry.

2',5'-Bis-O-(tert-butyldimethylsilyl)-3'-spiro-5''-(4''-amino-1'',2''- oxathiole-2'',2'-dioxide)pyrimidine (TSAO) nucleoside analogues: highlyselective inhibitors of human immunodeficiency virus type 1 that are targeted at the viral reverse transcriptase.

E. De Clercq, A. Vandamme, C. Perno, 1992, Proceedings of the National Academy of Sciences of the United States of America.

TSAO analogues. 3. Synthesis and anti-HIV-1 activity of 2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl 3'-spiro-5''-(4''-amino-1'',2''-oxathiole 2'',2''-dioxide) purine and purine-modified nucleosides.

E. De Clercq, J. Balzarini, M. Camarasa, 1993, Journal of medicinal chemistry.

Dimerization inhibitors of HIV-1 reverse transcriptase, protease and integrase: a single mode of inhibition for the three HIV enzymes?

F. Gago, M. Camarasa, S. Velázquez, 2006, Antiviral research.

TSAO compounds: the comprehensive story of a unique family of HIV-1 specific inhibitors of reverse transcriptase.

F. Gago, J. Balzarini, M. Camarasa, 2004, Current topics in medicinal chemistry.

Anti-HIV-1 activity of a tripodal receptor that recognizes mannose oligomers.

Y. Pommier, J. Balzarini, S. Noppen, 2015, European journal of medicinal chemistry.

Differential Recognition of Mannose‐Based Polysaccharides by Tripodal Receptors Based on a Triethylbenzene Scaffold Substituted with Trihydroxybenzoyl Moieties

M. Camarasa, A. Ardá, A. Prieto, 2013 .

Improving the antiviral efficacy and selectivity of HIV-1 reverse transcriptase inhibitor TSAO-T by the introduction of functional groups at the N-3 position.

E. De Clercq, F. Gago, J. Balzarini, 2005, Journal of medicinal chemistry.

Unprecedented lability of the 5'-O-tert-butyldimethylsilyl group from 3'-spiro-5''-(4''-acylamino-1'',2''-oxathiole-2'',2''-dioxide) nucleoside derivatives via neighboring group participation of the 4''-acylamino residue.

Á. Lozano, M. Camarasa, S. Velázquez, 2006, Journal of Organic Chemistry.

Novel [2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl]- 3'-spiro-5''-(4''-amino-1'',2''-oxathiole-2'',2" -dioxide) derivatives with anti-HIV-1 and anti-human-cytomegalovirus activity.

E. De Clercq, J. Balzarini, M. Camarasa, 2005, Journal of medicinal chemistry.

3'-Spiro nucleosides, a new class of specific human immunodeficiency virus type 1 inhibitors: synthesis and antiviral activity of [2'-5'-bis-O-(tert-butyldimethylsilyl)-beta-D-xylo- and -ribofuranose]-3'-spiro-5"-[4"-amino-1",2"-oxathiole 2",2"-dioxide] (TSAO) pyrimidine nucleosides.

E. De Clercq, J. Balzarini, E. Clercq, 1992, Journal of medicinal chemistry.

Novel series of TSAO-T derivatives. Synthesis and anti-HIV-1 activity of 4-, 5-, and 6-substituted pyrimidine analogues.

E. De Clercq, J. Balzarini, M. Camarasa, 1994, Journal of medicinal chemistry.

Improving the selectivity of acyclic nucleoside analogues as inhibitors of human mitochondrial thymidine kinase: replacement of a triphenylmethoxy moiety with substituted amines and carboxamides.

F. Gago, J. Balzarini, A. Karlsson, 2003, Bioorganic & medicinal chemistry letters.

TSAO Analogues. Stereospecific Synthesis and Anti‐HIV‐1 Activity of 1‐( 2′,5′‐Bis‐O‐(tert‐butyldimethylsilyl)‐β‐D‐ribofuranosyl)‐3′‐spiro‐ 5′′‐(4′′‐amino‐1′′,2′′‐oxathiole 2′′,2′′‐dioxide)pyrimidine and Pyrimidine‐Modified Nucleosides.

J. Balzarini, E. Clercq, M. Camarasa, 1992 .

3′-Spiro Nucleosides, a New Class of Specific Human Immunodeficiency Virus Type 1 Inhibitors: Synthesis and Antiviral Activity of (2′,5′- Bis-O-(tert-butyldimethylsilyl)-β-D-xylo- and -ribofuranose)-3′- spiro-5′′-(4′′-amino-1′′,2′′-oxathiole 2′′,2′′-Dioxide) (TSAO) Pyrimidine Nucleosides.

J. Balzarini, E. Clercq, M. Camarasa, 1992 .

TSAO analogues. Stereospecific synthesis and anti-HIV-1 activity of 1-[2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl]-3'-spiro -5''- (4''-amino-1'',2''-oxathiole 2'',2''-dioxide) pyrimidine and pyrimidine-modified nucleosides.

E. De Clercq, J. Balzarini, M. Camarasa, 1992, Journal of medicinal chemistry.

Hiv-1 Specific Reverse Transcriptase Inhibitors: why are Tsao-Nucleosides so Unique?

E. De Clercq, F. Gago, J. Balzarini, 2000 .

Metabolism and pharmacokinetics of the anti-HIV-1-specific inhibitor [1-[2′,5′-Bis-O-(tert-butyldimethylsilyl)-β-d-ribofuranosyl]-3-N-methyl-thymine]-3′-spiro-5″-(4″-amino-1″,2″-oxathiole-

L. Naesens, J. Balzarini, E. Clercq, 1993 .

Kinetics of inhibition of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase by the novel HIV-1-specific nucleoside analogue [2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl]-3'-spiro-5 "- (4"-amino-1",2"-oxathiole-2",2"-dioxide)thymine (TSAO-T).

E. De Clercq, P. Barr, J. Balzarini, 1992, The Journal of biological chemistry.

N-3 Substituted TSAO Derivatives as a Probe to Explore the Dimeric Interface of HIV-1 Reverse Transcriptase

E. De Clercq, J. Balzarini, M. Camarasa, 2003, Nucleosides, Nucleotides & Nucleic Acids.

Identification of a putative binding site for [2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl]-3'-spiro-5''-(4''-amino-1'',2''-oxathiole-2'',2''-dioxide)thymine (TSAO) derivatives at the p51-p66 interface of HIV-1 reverse transcriptase.

F. Gago, J. Balzarini, M. Camarasa, 2001, Journal of medicinal chemistry.

Identification of a novel family of nucleosides that specifically inhibit HIV-1 reverse transcriptase.

E. De Clercq, J. Balzarini, M. Camarasa, 2001, Bioorganic & Medicinal Chemistry Letters.

Exploitation of the Low Fidelity of Human Immunodeficiency Virus Type 1 (HIV-1) Reverse Transcriptase and the Nucleotide Composition Bias in the HIV-1 Genome To Alter the Drug Resistance Development of HIV

Jan Balzarini, Anna Karlsson, E. De Clercq, 2001, Journal of Virology.

4″-H-TSAO-T, A NOVEL PROTOTYPE IN THE HIV-1 SPECIFIC TSAO FAMILY

E. De Clercq, J. Balzarini, M. Camarasa, 2001, Nucleosides, nucleotides & nucleic acids.

“SECOND GENERATION” OF TSAO COMPOUNDS DIRECTED AGAINST HIV-1 TSAO-RESISTANT STRAINS

E. De Clercq, J. Balzarini, M. Camarasa, 2001, Nucleosides, nucleotides & nucleic acids.

Site-directed mutagenesis of human immunodeficiency virus type 1 reverse transcriptase at amino acid position 138.

A. Aertsen, E. De Clercq, A. Vandamme, 2001, Virology.

TSAO-T Analogues Bearing Amino Acids at Position N-3 of Thymine: Synthesis and Anti-Human Immunodeficiency Virus Activity

E. De Clercq, J. Balzarini, C. Chamorro, 2000, Antiviral chemistry & chemotherapy.

Synthesis of Novel 5″-Substituted Tsao-T Analogues with Anti-Hiv-1 Activity

E. De Clercq, J. Balzarini, M. Camarasa, 2000 .

Novel Tsao Derivatives. Synthesis and Anti-HIV-1 Activity of Allofuranosyl-TSAO-T Analogues ‡

J. Balzarini, E. Clercq, M. Camarasa, 1996 .

Novel N-3 Substituted TSAO-T Derivatives: Synthesis and Anti-HIV-Evaluation

J. Balzarini, M. Camarasa, N. Sluis-Cremer, 2008, Nucleosides, nucleotides & nucleic acids.

Structure-Activity Relationship Studies on a Novel Family of Specific HIV-1 Reverse Transcriptase Inhibitors

E. De Clercq, J. Balzarini, M. Camarasa, 2003, Antiviral chemistry & chemotherapy.

Analogues of TSAO-T as the First Sugar Derivatives That Specifically Inhibit HIV-1 Reverse Transcriptase

F. Gago, J. Perez-Perez, J. Balzarini, 1998 .

Steric and Electronic Properties of the 3′-spiro Moiety of TSAO-T and Analogues

Á. Lozano, M. Camarasa, M. Jimeno, 1999 .

Abasic analogues of TSAO-T as the first sugar derivatives that specifically inhibit HIV-1 reverse transcriptase.

E. De Clercq, F. Gago, J. Balzarini, 1998, Journal of medicinal chemistry.

Synthesis of [1-[2′,5′-bis-O-(t-Butyldimethylsilyl)-β- L-ribofuranosyl] thymine]-3′-spiro-5″-(4″-amino-1″,2″-oxathiole-2″,2″-dioxide) (L-TSAO-T)

J. Balzarini, E. Clercq, S. Ingate, 1995 .

Human immunodeficiency virus type 1 (HIV-1) strains selected for resistance against the HIV-1-specific [2',5'-bis-O-(tert-butyldimethylsilyl)-3'-spiro- 5''-(4''-amino-1'',2''-oxathiole-2'',2''-dioxide)]-beta-D-pentofurano syl (TSAO) nucleoside analogues retain sensitivity to HIV-1-specific nonnucleo

L. Vrang, A. Vandamme, B. Oberg, 1993, Proceedings of the National Academy of Sciences of the United States of America.

Unexpected Results in the Reaction of 5′-Tosyl TSAO-m3T With Amines

F. Gago, A. Esteban-Gamboa, J. Balzarini, 1999 .

Pharmacological Elevation of Cellular Dihydrosphingomyelin Provides a Novel Antiviral Strategy against West Nile Virus Infection

J. Saiz, M. Martín-Acebes, E. Escribano-Romero, 2022, bioRxiv.

N‐3 Substituted TSAO Derivatives as a Probe to Explore the Dimeric Interface of HIV‐1 Reverse Transcriptase

J. Balzarini, E. Clercq, M. Camarasa, 2004 .

Human immunodeficiency virus type 1-specific [2',5'-bis-O-(tert- butyldimethylsilyl)-beta-D-ribofuranosyl]-3'-spiro-5"-(4"-amino-1",2"- oxathiole-2",2"-dioxide)-purine analogues show a resistance spectrum that is different from that of the human immunodeficiency virus type 1-specific non-nucleoside

E. De Clercq, J. Balzarini, A. Karlsson, 1993, Molecular pharmacology.

Design and discovery of a novel dipeptidyl-peptidase IV (CD26)-based prodrug approach.

I. De Meester, J. Balzarini, M. Camarasa, 2006, Journal of medicinal chemistry.

Synthesis of novel Bi-, Tri-, and tetracyclic nucleosides by reaction of a common cyclic enamine derived from TSAO-T with nucleophiles.

M. Camarasa, M. Jimeno, C. Chamorro, 2004, The Journal of organic chemistry.

Synthesis of Novel 5′-Substituted TSAO-T Analogues with anti-HIV-1 Activity.

J. Balzarini, E. Clercq, M. Camarasa, 2000 .

Novel TSAO Derivatives. Synthesis and Anti-HIV-1 Activity of Allofuranosyl-TSAO-T Analogues.

J. Balzarini, E. Clercq, M. Camarasa, 1996 .

Novel N‐3 Substituted Tsao‐T Derivatives: Synthesis and anti‐HIV‐Evaluation.

J. Balzarini, M. Camarasa, N. Sluis-Cremer, 2008 .

Suppression of the breakthrough of human immunodeficiency virus type 1 (HIV-1) in cell culture by thiocarboxanilide derivatives when used individually or in combination with other HIV-1-specific inhibitors (i.e., TSAO derivatives).

E. De Clercq, J. Balzarini, A. Karlsson, 1995, Proceedings of the National Academy of Sciences of the United States of America.

Tryptophan Trimers and Tetramers Inhibit Dengue and Zika Virus Replication by Interfering with Viral Attachment Processes

C. Pannecouque, D. Schols, S. Noppen, 2020, Antimicrobial Agents and Chemotherapy.

Organotropic dendrons with high potency as HIV-1, HIV-2 and EV-A71 cell entry inhibitors.

F. Gago, J. Neyts, D. Schols, 2022, European journal of medicinal chemistry.

A SCAFFOLD SIMPLIFICATION STRATEGY LEADS TO A NOVEL GENERATION OF DUAL HUMAN IMMUNODEFICIENCY VIRUS AND ENTEROVIRUS-A71 ENTRY INHIBITORS.

F. Gago, S. Hafenstein, L. Delang, 2019, Journal of medicinal chemistry.

Optimization of a Class of Tryptophan Dendrimers That Inhibit HIV Replication Leads to a Selective, Specific, and Low-Nanomolar Inhibitor of Clinical Isolates of Enterovirus A71

L. Delang, J. Neyts, M. Camarasa, 2016, Antimicrobial Agents and Chemotherapy.

Tryptophan dendrimers that inhibit HIV replication, prevent virus entry and bind to the HIV envelope glycoproteins gp120 and gp41.

Jan Balzarini, Ignacio Colomer, J. Balzarini, 2015, European journal of medicinal chemistry.

Insertion of an Amphipathic Linker in a Tetrapodal Tryptophan Derivative Leads to a Novel and Highly Potent Entry Inhibitor of Enterovirus A71 Clinical Isolates

F. Gago, J. Neyts, D. Schols, 2023, International Journal of Molecular Sciences.

Multivalent Tryptophan‐ and Tyrosine‐Containing [60]Fullerene Hexa‐Adducts as Dual HIV and Enterovirus A71 Entry Inhibitors

F. Gago, J. Neyts, N. Martín, 2021, Chemistry.

Novel Polyphenols That Inhibit Colon Cancer Cell Growth Affecting Cancer Cell Metabolism

A. Ramírez de Molina, G. Reglero, M. Gómez de Cedrón, 2018, The Journal of Pharmacology and Experimental Therapeutics.

Peptidoglycan editing in non-proliferating intracellular Salmonella as source of interference with immune signaling

F. Cava, S. Velázquez, M. Pucciarelli, 2022, PLoS pathogens.

Novel series of [ddN]-[TSAO-T] heterodimers as potential bi-functional inhibitors of HIV-1 RT. Studies in the linker and ddN region.

E. De Clercq, A. Esteban-Gamboa, J. Balzarini, 1999, Nucleosides and Nucleotides.

Marked inhibitory activity of non-nucleoside reverse transcriptase inhibitors against human immunodeficiency virus type 1 when combined with (-)2',3'-dideoxy-3'-thiacytidine.

E. De Clercq, J. Balzarini, A. Karlsson, 1996, Molecular pharmacology.