Does the 2-methylthiomethyl substituent really confer high anti-HIV-1 activity to S-DABOS?

Authors
Sbardella, G Mai, A Artico, M Massa, S Marceddu, T Vargiu, L Marongiu, ME La Colla, P
Citation
G. Sbardella et al., Does the 2-methylthiomethyl substituent really confer high anti-HIV-1 activity to S-DABOS?, MED CHEM RE, 10(1), 2000, pp. 30-39
Citations number
22
Categorie Soggetti
Chemistry & Analysis
Journal title
MEDICINAL CHEMISTRY RESEARCH
ISSN journal
10542523 → ACNP
Volume
10
Issue
1
Year of publication
2000
Pages
30 - 39
Database
ISI
SICI code
1054-2523(2000)10:1<30:DT2SRC>2.0.ZU;2-4
Abstract
S-DABO derivatives containing the methylthiomethyl (MTM) group have been sy nthesized and tested for anti-HIV-1 activity in cell-based assay (MTT and p 24 assays) and for their capability to target the HIV-1 reverse transcripta se in enzyme assays. Data of experiments lead to the conclusion that the in troduction of a 2-MTM-thio side chain is not sufficient per se to significa ntly increase S-DABO's potency. Nevertheless, potent MTM-S-DABOs can be obt ained by introducing a 2,6- difluorophenylmethyl moiety as a C-6 substituen t.