The effects of sulfonic acid-related compounds on the cytopathicity of HIV.
Int Conf AIDS 1990 Jun 20-23; 6:332 (abstract no. 1074) Clanton DJ, Weislow O, McMahon J, Schultz R, Narayanan V, Bader J, Boyd M; Developmental Therapeutics Program, Division of Cancer Treatment, National Cancer Institute, National Institute of Health, Bethesda, MD, USA
The AIDS antiviral screening program of the National Cancer Institute has tested 12,000 compounds acquired from various sources worldwide (a description of this program will be reviewed). In the course of this screening, many compounds with sulfonic acid groups were found to be active. Sulfonic acid compounds exhibiting anti-HIV activity, including several structurally related to suramin, were tested under identical conditions in a comparative study. Several of these compounds were active in a range (2.0-20.0 uM) considered encouraging for further study. One compound, Direct Orange NSC#007229, was selected on the basis of its low effective concentration (EC50=6.6 uM) and minimal toxicity (IC50 greater than 145 uM). Results of our studies on this compound, including its mechanism of action, cytotoxicity, and affects of the drug on virus particles, will be presented, and they suggest that this compound may be useful in the therapeutic intervention against HIV infection.
Keywords: AEGIS, HIV, Sulfonic Acids, Acquired Immunodeficiency Syndrome, Reverse Transcriptase Inhibitors, Antiviral Agents, Anti-HIV Agents, HIV-1 Reverse Transcriptase, Suramin, Indicators and Reagents, ICA6