Article
New alkenyldiarylmethanes with enhanced potencies as anti-HIV agents which act as non-nucleoside reverse transcriptase inhibitors.
Journal of medicinal chemistry - 4 Jun 1998
Cushman M, Casimiro-Garcia A, Hejchman E, Ruell J A, Huang M, Schaeffer C A, Williamson K, Rice W G, Buckheit R W
Abstract excerpt
Twenty-two new alkenyldiarylmethanes (ADAMs) were synthesized and evaluated for inhibition of HIV-1 replication. The most potent compound proved to be methyl 3',3"-dichloro-4',4"-dimethoxy-5', 5"-bis(methoxycarbonyl)-6,6-diphenyl-5-hexenoate (ADAM II), which displayed an EC50 of 13 nM for inhibit...
Topics
- Alkanes
- Animals
- Anti-HIV Agents
- Binding Sites
- Caproates
- Cell Line
- Cytopathogenic Effect, Viral
- Drug Evaluation, Preclinical
- Drug Resistance, Microbial
- HIV Reverse Transcriptase
- HIV-1
- Leukocytes, Mononuclear
- Macrophages
- Mice
