Reference

Both 2',3'-dideoxythymidine and its 2',3'-unsaturated derivative (2',3'-dideoxythymidinene) are potent and selective inhibitors of human immunodeficiency virus replication in vitro

Both 2',3'-dideoxythymidine and its 2',3'-unsaturated derivative (2',3'-dideoxythymidinene) are potent and selective inhibitors of human immunodeficiency virus replication in vitro. Baba, Masanori; Pauwels, Rudi; Herdewijn, Piet; De Clercq, Erik; Desmyter, Jan; Vandeputte, Michel (Rega Inst. Med. Res., Kathol. Univ. Leuven, Louvain B-3000, Belg.). Biochem. Biophys. Res. Commun., 142(1), 128-34 (English) 1987. CODEN: BBRCA9. ISSN: 0006-291X.Several substances with their cas registry numbers 5974-93-6 and 4097-22-7 may be metioned in this study. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Section cross-reference(s): 10, 15 2',3'-Dideoxythymidine (ddThd) [3416-05-5] and its 2',3'-unsatd. deriv., 2',3'-dideoxythymidinene (ddeThd) [3056-17-5], are potent and selective inhibitors of human immunodeficiency virus (HIV) in vitro. When evaluated for their inhibitory effects on the cytopathogenicity of HIV in MT-4 cells, ddThd and ddeThd completely protected the cells against destruction by the virus at a concn. of 1 and 0.04 mM, resp. In this aspect, ddeThd was ~5-fold more potent than 2',3'-dideoxycytidine (ddCyd) [7481-89-2], one of the most potent and selective anti-HIV compds. now pursued for its therapeutic potential in the treatment of AIDS. Both ddThd and ddeThd also suppressed HIV antigen expression at 1 and 0.04 mM, resp. Their selectivity indexes, as based on the ratio of the 50% cytotoxic dose to the 50% antiviral ED, were 120 (ddeThd) and >625 (ddThd). .

In vitro activity of stampidine against primary clinical human immunodeficiency virus isolates

In vitro activity of stampidine against primary clinical human immunodeficiency virus isolates. Uckun, Fatih M.; Pendergrass, Sharon; Qazi, Sanjive; Venkatachalam, Taracad K. (Drug Discovery Program, Departments of Virology, Bioinformatics, Immunology, and Chemistry, Parker Hughes Cancer Center, St. Paul, MN, USA). Arzneimittel Forschung, 54(1), 69-77 (English) 2004 Editio Cantor Verlag. CODEN: ARZNAD. ISSN: 0004-4172. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) The in vitro activity profile of stampidine (CAS 217178-62-6, STAMP) was examd. against clin. isolates of HIV-1. In a side-by-side comparison against 10 zidovudine-sensitive clin. HIV-1 isolates, STAMP was 100-fold more potent than stavudine (CAS 3056-17-5) and twice as effective as zidovudine (CAS 30516-87-1). STAMP was also active against phenotypically and/or genotypically NRTI (nucleoside analog inhibitors of reverse transcriptase)-resistant HIV and inhibited the replication of 20 zidovudine-resistant clin. HIV-1 isolates with low nanomolar to subnanomolar IC50 values. Similarly, STAMP inhibited the replication of 9 genotypically NNRTI (non-nucleoside analog inhibitors of reverse transcriptase)-resistant clin. HIV-1 isolates (n = 9) with an av. IC50 value of 11.2 ± 6.5 nmol/L. The remarkable potency of STAMP against clin. HIV-1 isolates with NRTI- or NNRTI-resistance warrants the further development of this promising new antiviral agent.