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María-Jesús Pérez-Pérez

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Chemicals & Drugs

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HIV-1
HIV-2

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Publications

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Sandra Liekens; Beatrice Nico; Ghislain Opdenakker; María-Jesús Pérez-Pérez; Jan Balzarini; Mirella Belleri; Annelies Bronckaers; Antonella Bugatti; Elena Casanova; Alba Gigante; Domenico Ribatti; Rebecca Sienaert; Marco Presta
The thymidine phosphorylase inhibitor 5'-O-tritylinosine (KIN59) is an antiangiogenic multitarget fibroblast growth factor-2 antagonist.
Leire Aguado; María-José Camarasa; María-Dolores Canela; Pieter Leyssen; Johan Neyts; Eva-María Priego; Hendrik Jan Thibaut; María-Jesús Pérez-Pérez
Efficient synthesis and anti-enteroviral activity of 9-arylpurines.
Virginia Lozano; Marleen Renders; Ana San-Félix; Dominique Schols; Leire Aguado; Jan Balzarini; María-José Camarasa; Bart Hoorelbeke; María-Jesús Pérez-Pérez
Targeting HIV entry through interaction with envelope glycoprotein 120 (gp120): synthesis and antiviral evaluation of 1,3,5-triazines with aromatic amino acids.

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All Publications

2012: Sandra Liekens; Beatrice Nico; Ghislain Opdenakker; María-Jesús Pérez-Pérez; Jan Balzarini; Mirella Belleri; Annelies Bronckaers; Antonella Bugatti; Elena Casanova; Alba Gigante; Domenico Ribatti; Rebecca Sienaert; Marco Presta
The thymidine phosphorylase inhibitor 5'-O-tritylinosine (KIN59) is an antiangiogenic multitarget fibroblast growth factor-2 antagonist.
Molecular cancer therapeutics 2012;11(4):817-29.
2012: Leire Aguado; María-José Camarasa; María-Dolores Canela; Pieter Leyssen; Johan Neyts; Eva-María Priego; Hendrik Jan Thibaut; María-Jesús Pérez-Pérez
Efficient synthesis and anti-enteroviral activity of 9-arylpurines.
European journal of medicinal chemistry 2012;49():279-88.
2011: Virginia Lozano; Marleen Renders; Ana San-Félix; Dominique Schols; Leire Aguado; Jan Balzarini; María-José Camarasa; Bart Hoorelbeke; María-Jesús Pérez-Pérez
Targeting HIV entry through interaction with envelope glycoprotein 120 (gp120): synthesis and antiviral evaluation of 1,3,5-triazines with aromatic amino acids.
Journal of medicinal chemistry 2011;54(15):5335-48.
2010: Olga Familiar; Hélène Munier-Lehmann; José Antonio Aínsa; María-José Camarasa; María-Jesús Pérez-Pérez
Design, synthesis and inhibitory activity against Mycobacterium tuberculosis thymidine monophosphate kinase of acyclic nucleoside analogues with a distal imidazoquinolinone.
European journal of medicinal chemistry 2010;45(12):5910-8.
2010: Elena Casanova; Eva-María Priego; María-Luisa Jimeno; Leire Aguado; Ana Negri; Federico Gago; María-José Camarasa; María-Jesús Pérez-Pérez
Intramolecular cation-pi interactions as the driving force to restrict the conformation of certain nucleosides.
The Journal of organic chemistry 2010;75(6):1974-81.
2010: Leire Aguado; Hendrik Jan Thibaut; Eva-María Priego; María-Luisa Jimeno; María-José Camarasa; Johan Neyts; María-Jesús Pérez-Pérez
9-Arylpurines as a novel class of enterovirus inhibitors.
Journal of medicinal chemistry 2010;53(1):316-24.
2009: Katrien O François; Christophe Pannecouque; Joeri Auwerx; Virginia Lozano; María-Jesús Pérez-Pérez; Dominique Schols; Jan Balzarini
The phthalocyanine prototype derivative Alcian Blue is the first synthetic agent with selective anti-human immunodeficiency virus activity due to its gp120 glycan-binding potential.
Antimicrobial agents and chemotherapy 2009;53(11):4852-9.
2009: A Bronckaers; L Aguado; A Negri; María-José Camarasa; Jan Balzarini; María-Jesús Pérez-Pérez; F Gago; S Liekens
Identification of aspartic acid-203 in human thymidine phosphorylase as an important residue for both catalysis and non-competitive inhibition by the small molecule "crystallization chaperone" 5'-O-tritylinosine (KIN59).
Biochemical pharmacology 2009;78(3):231-40.
2009: Leire Aguado; María-José Camarasa; María-Jesús Pérez-Pérez
Microwave-assisted synthesis of 9-arylpurines.
Journal of combinatorial chemistry 2009;11(2):210-2.
2009: Virginia Lozano; Rebeca Hernández; Carmen Mijangos; María-Jesús Pérez-Pérez
A novel organogelator incorporating tert-butyl esters of asparagines.
Organic & biomolecular chemistry 2009;7(2):364-9.
2008: María-Jesús Pérez-Pérez; Eva-María Priego; Ana-Isabel Hernández; Olga Familiar; María-José Camarasa; Ana Negri; Federico Gago; Jan Balzarini
Structure, physiological role, and specific inhibitors of human thymidine kinase 2 (TK2): present and future.
Medicinal research reviews 2008;28(5):797-820.
2008: Olga Familiar; Hélène Munier-Lehmann; Ana Negri; Federico Gago; Dominique Douguet; Leen Rigouts; Ana-Isabel Hernández; María-José Camarasa; María-Jesús Pérez-Pérez
Exploring acyclic nucleoside analogues as inhibitors of Mycobacterium tuberculosis thymidylate kinase.
ChemMedChem 2008;3(7):1083-93.
2008: María-Cruz Bonache; Ernesto Quesada; Chih-Wei Sheen; Jan Balzarini; Nicolas Sluis-Cremer; María-Jesús Pérez-Pérez; María-José Camarasa; Ana San-Félix
Novel N-3 substituted TSAO-T derivatives: synthesis and anti-HIV-evaluation.
Nucleosides, nucleotides & nucleic acids 2008;27(4):351-67.
2008: Eva-María Priego; María-Jesús Pérez-Pérez; Jacobien K von Frijtag Drabbe Kuenzel; Henk de Vries; Adriaan P IJzerman; María-José Camarasa; Sonsoles Martín-Santamaría
Selective human adenosine A3 antagonists based on pyrido[2,1-f]purine-2,4-diones: novel features of hA3 antagonist binding.
ChemMedChem 2008;3(1):111-9.
2007: Sandra Liekens; Annelies Bronckaers; María-Jesús Pérez-Pérez; Jan Balzarini
Targeting platelet-derived endothelial cell growth factor/thymidine phosphorylase for cancer therapy.
Biochemical pharmacology 2007;74(11):1555-67.
2007: Elena Casanova; Leire Aguado; María-Luisa Jimeno; Federico Gago; María-José Camarasa; María-Jesús Pérez-Pérez
7,5'-O-dibenzylinosines: synthesis and studies on their conformational properties.
Nucleosides, nucleotides & nucleic acids 2007;26(6-7):695-9.
2006: Ana-Isabel Hernandez; Olga Familiar; Ana Negri; Fátima Rodríguez-Barrios; Federico Gago; Anna Karlsson; María-José Camarasa; Jan Balzarini; María-Jesús Pérez-Pérez
N1-substituted thymine derivatives as mitochondrial thymidine kinase (TK-2) inhibitors.
Journal of medicinal chemistry 2006;49(26):7766-73.
2006: Kamel El Omari; Annelies Bronckaers; Sandra Liekens; María-Jesús Pérez-Pérez; Jan Balzarini; David K Stammers
Structural basis for non-competitive product inhibition in human thymidine phosphorylase: implications for drug design.
The Biochemical journal 2006;399(2):199-204.
2006: Elena Casanova; Ana-Isabel Hernandez; Eva-María Priego; Sandra Liekens; María-José Camarasa; Jan Balzarini; María-Jesús Pérez-Pérez
5'-O-tritylinosine and analogues as allosteric inhibitors of human thymidine phosphorylase.
Journal of medicinal chemistry 2006;49(18):5562-70.
2006: María-José Camarasa; Sonsoles Velázquez; Ana San-Félix; María-Jesús Pérez-Pérez; Federico Gago
Dimerization inhibitors of HIV-1 reverse transcriptase, protease and integrase: a single mode of inhibition for the three HIV enzymes?
Antiviral research 2006;71(2-3):260-7.
2006: Sandra Liekens; Annelies Bronckaers; Ana-Isabel Hernández; Eva-María Priego; Elena Casanova; María-José Camarasa; María-Jesús Pérez-Pérez; Jan Balzarini
5'-O-tritylated nucleoside derivatives: inhibition of thymidine phosphorylase and angiogenesis.
Molecular pharmacology 2006;70(2):501-9.
2006: Elisa Franzolin; Chiara Rampazzo; María-Jesús Pérez-Pérez; Ana-Isabel Hernández; Jan Balzarini; Vera Bianchi
Bromovinyl-deoxyuridine: A selective substrate for mitochondrial thymidine kinase in cell extracts.
Biochemical and biophysical research communications 2006;344(1):30-6.
2006: Sonia De Castro; Angel Lozano; María-Luisa Jimeno; María-Jesús Pérez-Pérez; Ana San-Félix; María-José Camarasa; Sonsoles Velázquez
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.
The Journal of organic chemistry 2006;71(4):1407-15.
2006: Sandra Liekens; Jan Balzarini; Ana-Isabel Hernández; Erik De Clercq; Eva-María Priego; María-José Camarasa; María-Jesús Pérez-Pérez
Thymidine phosphorylase is noncompetitively inhibited by 5'-O-trityl-inosine (KIN59) and related compounds.
Nucleosides, nucleotides & nucleic acids 2006;25(9-11):975-80.
2006: María-José Camarasa; Sonsoles Velázquez; Ana San-Félix; María-Jesús Pérez-Pérez; María-Cruz Bonache; Sonia De Castro
TSAO derivatives, inhibitors of HIV-1 reverse transcriptase dimerization: recent progress.
Current pharmaceutical design 2006;12(15):1895-907.
2005: María-Jesús Pérez-Pérez; Eva-María Priego; Ana-Isabel Hernández; María-José Camarasa; Jan Balzarini; Sandra Liekens
Thymidine phosphorylase inhibitors: recent developments and potential therapeutic applications.
Mini reviews in medicinal chemistry 2005;5(12):1113-23.
2005: Sonia De Castro; Esther Lobatón; María-Jesús Pérez-Pérez; Ana San-Félix; Alessandra Cordeiro; Graciela Andrei; Robert Snoeck; Erik De Clercq; Jan Balzarini; María-José Camarasa; Sonsoles Velázquez
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.
Journal of medicinal chemistry 2005;48(4):1158-68.
2005: María-Jesús Pérez-Pérez; Ana-Isabel Hernández; Eva-María Priego; Fátima Rodríguez-Barrios; Federico Gago; María-José Camarasa; Jan Balzarini
Mitochondrial thymidine kinase inhibitors.
Current topics in medicinal chemistry 2005;5(13):1205-19.
2005: María-José Camarasa; Sonsoles Velázquez; Ana San-Félix; María-Jesús Pérez-Pérez
TSAO derivatives the first non-peptide inhibitors of HIV-1 RT dimerization.
Antiviral chemistry & chemotherapy 2005;16(3):147-53.
2004: Eva-María Priego; Jan Balzarini; Anna Karlsson; María-José Camarasa; María-Jesús Pérez-Pérez
Synthesis and evaluation of thymine-derived carboxamides against mitochondrial thymidine kinase (TK-2) and related enzymes.
Bioorganic & medicinal chemistry 2004;12(19):5079-90.
2004: Sandra Liekens; Ana-Isabel Hernández; Dragana Vukasovic; Erik De Clercq; María-José Camarasa; María-Jesús Pérez-Pérez; Jan Balzarini
The nucleoside derivative 5'-O-trityl-inosine (KIN59) suppresses thymidine phosphorylase-triggered angiogenesis via a noncompetitive mechanism of action.
The Journal of biological chemistry 2004;279(28):29598-605.
2004: Jesús Mendieta; Sonsoles Martín-Santamaría; Eva-María Priego; Jan Balzarini; María-José Camarasa; María-Jesús Pérez-Pérez; Federico Gago
Role of histidine-85 in the catalytic mechanism of thymidine phosphorylase as assessed by targeted molecular dynamics simulations and quantum mechanical calculations.
Biochemistry 2004;43(2):405-14.
2004: María-José Camarasa; Ana San-Félix; Sonsoles Velázquez; María-Jesús Pérez-Pérez; Federico Gago; Jan Balzarini
TSAO compounds: the comprehensive story of a unique family of HIV-1 specific inhibitors of reverse transcriptase.
Current topics in medicinal chemistry 2004;4(9):945-63.
2003: Ana-Isabel Hernández; Jan Balzarini; Fátima Rodríguez-Barrios; Ana San-Félix; Anna Karlsson; Federico Gago; María-José Camarasa; María-Jesús Pérez-Pérez
Improving the selectivity of acyclic nucleoside analogues as inhibitors of human mitochondrial thymidine kinase: replacement of a triphenylmethoxy moiety with substituted amines and carboxamides.
Bioorganic & medicinal chemistry letters 2003;13(18):3027-30.
2003: Cristina Chamorro; Santos M Luengo; María-Cruz Bonache; Sonsoles Velázquez; María-Jesús Pérez-Pérez; María-José Camarasa; Federico Gago; María-Luisa Jimeno; Ana San-Félix
Synthesis and structural characterization of pyrimidine bi- and tricyclic nucleosides with sugar puckers conformationally locked into the eastern region of the pseudorotational cycle.
The Journal of organic chemistry 2003;68(17):6695-704.
2003: Sonia De Castro; María-Jesús Pérez-Pérez; Esther Lobatón; Erik De Clercq; Jan Balzarini; María-José Camarasa; Sonsoles Velázquez
Unusual lability of 5'-O-tert-butyldimethylsilyl group on 4''-acyl TSAO derivatives.
Nucleosides, nucleotides & nucleic acids 2003;22(5-8):959-61.
2003: Eva-María Priego; Jesús Mendieta; Federico Gago; Jan Balzarini; Erik De Clercq; María-José Camarasa; María-Jesús Pérez-Pérez
Towards new thymidine phosphorylase/PD-ECGF inhibitors based on the transition state of the enzyme reaction.
Nucleosides, nucleotides & nucleic acids 2003;22(5-8):951-3.
2003: Jan Balzarini; Ana-Isabel Hernández; Philippe Roche; Robert M Esnouf; Anna Karlsson; María-José Camarasa; María-Jesús Pérez-Pérez
Non-nucleoside inhibitors of mitochondrial thymidine kinase (TK-2) differentially inhibit the closely related herpes simplex virus type 1 TK and Drosophila melanogaster multifunctional deoxynucleoside kinase.
Molecular pharmacology 2003;63(2):263-70.
2002: Ana-Isabel Hernández; Jan Balzarini; Anna Karlsson; María-José Camarasa; María-Jesús Pérez-Pérez
Acyclic nucleoside analogues as novel inhibitors of human mitochondrial thymidine kinase.
Journal of medicinal chemistry 2002;45(19):4254-63.
2002: Esther Lobatón; Fátima Rodríguez-Barrios; Federico Gago; María-Jesús Pérez-Pérez; Erik De Clercq; Jan Balzarini; María-José Camarasa; Sonsoles Velázquez
Synthesis of 3' '-substituted TSAO derivatives with anti-HIV-1 and anti-HIV-2 activity through an efficient palladium-catalyzed cross-coupling approach.
Journal of medicinal chemistry 2002;45(18):3934-45.
2002: Eva-María Priego; Jacobien von Frijtag Drabbe Kuenzel; Adriaan P IJzerman; María-José Camarasa; María-Jesús Pérez-Pérez
Pyrido[2,1-f]purine-2,4-dione derivatives as a novel class of highly potent human A(3) adenosine receptor antagonists.
Journal of medicinal chemistry 2002;45(16):3337-44.
2002: Sandra Liekens; Filip Bilsen; Erik De Clercq; Eva-María Priego; María-José Camarasa; María-Jesús Pérez-Pérez; Jan Balzarini
Anti-angiogenic activity of a novel multi-substrate analogue inhibitor of thymidine phosphorylase.
FEBS letters 2002;510(1-2):83-8.
2001: Jan Balzarini; María-José Camarasa; María-Jesús Pérez-Pérez; Ana San-Félix; Sonsoles Velázquez; Carlo Federico Perno; Erik De Clercq; J N Anderson; Anna Karlsson
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.
Journal of virology 2001;75(13):5772-7.
2001: Fátima Rodríguez-Barrios; C Pérez; Esther Lobatón; Sonsoles Velázquez; Cristina Chamorro; Ana San-Félix; María-Jesús Pérez-Pérez; María-José Camarasa; H Pelemans; Jan Balzarini; Federico Gago
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.
Journal of medicinal chemistry 2001;44(12):1853-65.
2001: Cristina Chamorro; María-Jesús Pérez-Pérez; Fátima Rodríguez-Barrios; Federico Gago; Erik De Clercq; Jan Balzarini; Ana San-Félix; María-José Camarasa
Exploring the role of the 5'-position of TSAO-T. Synthesis and anti-HIV evaluation of novel TSAO-T derivatives.
Antiviral research 2001;50(3):207-22.
2001: Esther Lobatón; Sonsoles Velázquez; María-Jesús Pérez-Pérez; María-Luisa Jimeno; Ana San-Félix; Erik De Clercq; Jan Balzarini; María-José Camarasa
"Second generation" of TSAO compounds directed against HIV-1 TSAO-resistant strains.
Nucleosides, nucleotides & nucleic acids 2001;20(4-7):707-10.
2001: H Pelemans; A Aertsen; Kristel Van Laethem; Anne-Mieke Vandamme; Erik De Clercq; María-Jesús Pérez-Pérez; Ana San-Félix; Sonsoles Velázquez; María-José Camarasa; Jan Balzarini
Site-directed mutagenesis of human immunodeficiency virus type 1 reverse transcriptase at amino acid position 138.
Virology 2001;280(1):97-106.
2000: Jan Balzarini; B Degrève; A Esteban-Gamboa; Robert M Esnouf; Erik De Clercq; Yves Engelborghs; María-José Camarasa; María-Jesús Pérez-Pérez
Kinetic analysis of novel multisubstrate analogue inhibitors of thymidine phosphorylase.
FEBS letters 2000;483(2-3):181-5.
2000: Jan Balzarini; C Zhu; Erik De Clercq; María-Jesús Pérez-Pérez; Cristina Chamorro; María-José Camarasa; A Karlsson
Novel ribofuranosylnucleoside lead compounds for potent and selective inhibitors of mitochondrial thymidine kinase-2.
The Biochemical journal 2000;351(Pt 1):167-71.
2000: Kristel Van Laethem; Jean-Claude Schmit; H Pelemans; Jan Balzarini; Myriam Witvrouw; María-Jesús Pérez-Pérez; María-José Camarasa; Robert M Esnouf; Stefano Aquaro; Alessandra Cenci; Carlo Federico Perno; Philippe Hermans; S Sprecher; Lidia Ruiz; Bonaventura Clotet; Eric Van Wijngaerden; Marc Van Ranst; Jan Desmyter; Erik De Clercq; Anne-Mieke Vandamme
Presence of 2',5'-Bis-O-(tert-butyldimethylsilyl)-3'-spiro-5"-(4"-amino-1",2"-oxath iole-2",2"-dioxide) (TSAO)-resistant virus strains in TSAO-inexperienced HIV patients.
AIDS research and human retroviruses 2000;16(9):825-33.
2000: A Esteban-Gamboa; Jan Balzarini; Robert M Esnouf; Erik De Clercq; María-José Camarasa; María-Jesús Pérez-Pérez
Design, synthesis, and enzymatic evaluation of multisubstrate analogue inhibitors of Escherichia coli thymidine phosphorylase.
Journal of medicinal chemistry 2000;43(5):971-83.
1999: Sonsoles Velázquez; V Tuñón; María-Luisa Jimeno; María-Jesús Pérez-Pérez; Ana San-Félix; Cristina Chamorro; Esther Lobatón; A Esteban-Gamboa; Erik De Clercq; Jan Balzarini; María-José Camarasa
Novel series of [ddN]-[TSAO-T] heterodimers as potential bi-functional inhibitors of HIV-1 RT. Studies in the linker and ddN region.
Nucleosides & nucleotides 1999;18(4-5):1029-30.
1999: Esther Lobatón; Sonsoles Velázquez; Ana San-Félix; Cristina Chamorro; V Tuñón; A Esteban-Gamboa; Erik De Clercq; Jan Balzarini; María-José Camarasa; María-Jesús Pérez-Pérez
Novel TSAO derivatives modified at positions 3" and 4" of the spiro moiety.
Nucleosides & nucleotides 1999;18(4-5):675-6.
1998: Sonsoles Velázquez; Cristina Chamorro; María-Jesús Pérez-Pérez; R Alvarez; María-Luisa Jimeno; A Martín-Domenech; C Pérez; Federico Gago; Erik De Clercq; Jan Balzarini; Ana San-Félix; María-José Camarasa
Abasic analogues of TSAO-T as the first sugar derivatives that specifically inhibit HIV-1 reverse transcriptase.
Journal of medicinal chemistry 1998;41(23):4636-47.
1998: Jan Balzarini; A E Gamboa; Robert M Esnouf; Sandra Liekens; Johan Neyts; Erik De Clercq; María-José Camarasa; María-Jesús Pérez-Pérez
7-Deazaxanthine, a novel prototype inhibitor of thymidine phosphorylase.
FEBS letters 1998;438(1-2):91-5.
1998: Cristina Chamorro; María-José Camarasa; María-Jesús Pérez-Pérez; Erik De Clercq; Jan Balzarini; Ana San-Félix
An approach towards the synthesis of potential metal-chelating TSAO-T derivatives as bidentate inhibitors of human immunodeficiency virus type 1 reverse transcriptase.
Antiviral chemistry & chemotherapy 1998;9(5):413-22.
1998: R Alvarez; María-Luisa Jimeno; Federico Gago; Jan Balzarini; María-Jesús Pérez-Pérez; María-José Camarasa
Novel 3'-spiro nucleoside analogues of TSAO-T. Part II. A comparative study based on NMR conformational analysis in solution and theoretical calculations.
Antiviral chemistry & chemotherapy 1998;9(4):333-40.
1996: Jan Balzarini; H Pelemans; María-Jesús Pérez-Pérez; Ana San-Félix; María-José Camarasa; E De Clercq; Anna Karlsson
Marked inhibitory activity of non-nucleoside reverse transcriptase inhibitors against human immunodeficiency virus type 1 when combined with (-)2',3'-dideoxy-3'-thiacytidine.
Molecular pharmacology 1996;49(5):882-90.
1995: Jan Balzarini; María-Jesús Pérez-Pérez; S Vélazquez; Ana San-Félix; María-José Camarasa; E De Clercq; Anna Karlsson
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).
Proceedings of the National Academy of Sciences of the United States of America 1995;92(12):5470-4.
1995: S Ingate; María-Jesús Pérez-Pérez; E De Clercq; Jan Balzarini; María-José Camarasa
Synthesis and anti-HIV-1 activity of novel TSAO-T derivatives modified at the 2'- and 5'-positions of the sugar moiety.
Antiviral research 1995;27(3):281-99.
1994: Ana San-Félix; Sonsoles Velázquez; María-Jesús Pérez-Pérez; Jan Balzarini; E De Clercq; María-José Camarasa
Novel series of TSAO-T derivatives. Synthesis and anti-HIV-1 activity of 4-, 5-, and 6-substituted pyrimidine analogues.
Journal of medicinal chemistry 1994;37(4):453-60.
1993: Sonsoles Velázquez; Ana San-Félix; María-Jesús Pérez-Pérez; Jan Balzarini; E De Clercq; María-José Camarasa
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.
Journal of medicinal chemistry 1993;36(22):3230-9.
1993: María-Jesús Pérez-Pérez; Jan Balzarini; E De Clercq; María-José Camarasa
Glycosyl-oxycarbonylaminosulfonyl-2',3'-dideoxynucleoside derivatives as lipophilic nucleotide mimics. Synthesis and anti-HIV activity.
Bioorganic & medicinal chemistry 1993;1(4):279-84.
1993: Jan Balzarini; Anna Karlsson; María-Jesús Pérez-Pérez; María-José Camarasa; E De Clercq
Knocking-out concentrations of HIV-1-specific inhibitors completely suppress HIV-1 infection and prevent the emergence of drug-resistant virus.
Virology 1993;196(2):576-85.
1993: Jan Balzarini; Anna Karlsson; María-Jesús Pérez-Pérez; María-José Camarasa; W G Tarpley; E De Clercq
Treatment of human immunodeficiency virus type 1 (HIV-1)-infected cells with combinations of HIV-1-specific inhibitors results in a different resistance pattern than does treatment with single-drug therapy.
Journal of virology 1993;67(9):5353-9.
1993: Jan Balzarini; Anna Karlsson; Anne-Mieke Vandamme; María-Jesús Pérez-Pérez; Hong Zhang; Lotta Vrang; B Oberg; Kristina Bäckbro; Torsten Unge; Ana San-Félix
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 nonnucleoside inhibitors.
Proceedings of the National Academy of Sciences of the United States of America 1993;90(15):6952-6.
1993: Jan Balzarini; Lieve Naesens; C Bohman; María-Jesús Pérez-Pérez; Ana San-Félix; María-José Camarasa; E De Clercq
Metabolism and pharmacokinetics of the anti-HIV-1-specific inhibitor [1-[2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl]-3-N- methyl-thymine]-3'-spiro-5''-(4''-amino-1'',2''-oxathiole-2'',2''-dio xide).
Biochemical pharmacology 1993;46(1):69-77.
1993: Jan Balzarini; Anna Karlsson; María-Jesús Pérez-Pérez; Lotta Vrang; J Walbers; Hong Zhang; B Oberg; Anne-Mieke Vandamme; María-José Camarasa; E De Clercq
HIV-1-specific reverse transcriptase inhibitors show differential activity against HIV-1 mutant strains containing different amino acid substitutions in the reverse transcriptase.
Virology 1993;192(1):246-53.
1992: María-Jesús Pérez-Pérez; Ana San-Félix; J Balzarini; E De Clercq; María-José Camarasa
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.
Journal of medicinal chemistry 1992;35(16):2988-95.
1992: María-José Camarasa; María-Jesús Pérez-Pérez; Ana San-Félix; J Balzarini; E De Clercq
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.
Journal of medicinal chemistry 1992;35(15):2721-7.
1992: Jan Balzarini; María-Jesús Pérez-Pérez; Ana San-Félix; María-José Camarasa; I C Bathurst; P J Barr; E De Clercq
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).
The Journal of biological chemistry 1992;267(17):11831-8.
1992: Jan Balzarini; María-Jesús Pérez-Pérez; Ana San-Félix; Dominique Schols; Carlo Federico Perno; Anne-Mieke Vandamme; María-José Camarasa; E De Clercq
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.
Proceedings of the National Academy of Sciences of the United States of America 1992;89(10):4392-6.
1992: Jan Balzarini; María-Jesús Pérez-Pérez; Ana San-Félix; S Velazquez; María-José Camarasa; E De Clercq
[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.
Antimicrobial agents and chemotherapy 1992;36(5):1073-80.