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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.
de Castro S, Lobatón E, Pérez-Pérez MJ, San-Félix A, Cordeiro A, Andrei G, Snoeck R, De Clercq E, Balzarini J, Camarasa MJ, Velázquez S. de Castro S, et al. Among authors: balzarini j. J Med Chem. 2005 Feb 24;48(4):1158-68. doi: 10.1021/jm040868q. J Med Chem. 2005. PMID: 15715482
The amino acid Asn136 in HIV-1 reverse transcriptase (RT) maintains efficient association of both RT subunits and enables the rational design of novel RT inhibitors.
Balzarini J, Auwerx J, Rodríguez-Barrios F, Chedad A, Farkas V, Ceccherini-Silberstein F, García-Aparicio C, Velázquez S, De Clercq E, Perno CF, Camarasa MJ, Gago F. Balzarini J, et al. Mol Pharmacol. 2005 Jul;68(1):49-60. doi: 10.1124/mol.105.012435. Epub 2005 Apr 15. Mol Pharmacol. 2005. PMID: 15833734
Structure-activity relationships of [2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl]- 3'-spiro-5' '-(4' '-amino-1' ',2' '-oxathiole-2' ',2' '-dioxide)thymine derivatives as inhibitors of HIV-1 reverse transcriptase dimerization.
Sluis-Cremer N, Hamamouch N, San Félix A, Velazquez S, Balzarini J, Camarasa MJ. Sluis-Cremer N, et al. Among authors: balzarini j. J Med Chem. 2006 Aug 10;49(16):4834-41. doi: 10.1021/jm0604575. J Med Chem. 2006. PMID: 16884295
We previously demonstrated that the N-3-ethyl derivative of 2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl]-3'-spiro-5' '-(4' '-amino-1' ',2' '-oxathiole-2' ',2' '-dioxide)thymine (TSAO-T) destabilizes the inter-subunit interactions of HIV-1 RT [Sluis-Cremer, N.; Dmie …
We previously demonstrated that the N-3-ethyl derivative of 2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl]-3'-spiro-5' '-(4' '- …
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.
Balzarini J, Pérez-Pérez MJ, San-Félix A, Schols D, Perno CF, Vandamme AM, Camarasa MJ, De Clercq E. Balzarini J, et al. Proc Natl Acad Sci U S A. 1992 May 15;89(10):4392-6. doi: 10.1073/pnas.89.10.4392. Proc Natl Acad Sci U S A. 1992. PMID: 1374900 Free PMC article.
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).
Balzarini J, Pérez-Pérez MJ, San-Félix A, Camarasa MJ, Bathurst IC, Barr PJ, De Clercq E. Balzarini J, et al. J Biol Chem. 1992 Jun 15;267(17):11831-8. J Biol Chem. 1992. PMID: 1376314 Free article.
1,243 results