Potent and selective activity of a new carbocyclic nucleoside analog (carbovir: NSC 614846) against human immunodeficiency virus in vitro.
Carbocyclic 2',3'-didehydro-2',3'-dideoxyguanosine (Carbovir: NSC 614846), a novel nucleoside analog, emerged as a potent and selective anti-HIV agent from a large screening program conducted by the National Cancer Institute and its contractors. Its hydrolytic stability and its ability to inhibit the infectivity and replication of HIV in T-cells at concentrations of approximately 200- to 400-fold below toxic concentrations make carbovir a top-priority candidate for development as a potential antiretroviral agent in the treatment of AIDS patients.
Vince
R
R
Department of Medicinal Chemistry, College of Pharmacy, University of Minnesota, Minneapolis 55455.
Hua
M
M
Brownell
J
J
Daluge
S
S
Lee
F C
FC
Shannon
W M
WM
Lavelle
G C
GC
Qualls
J
J
Weislow
O S
OS
Kiser
R
R
D000163:Acquired Immunodeficiency Syndrome / Q000188:drug therapy; D000998:Antiviral Agents; D003588:Cytopathogenic Effect, Viral / Q000187:drug effects; D015224:Dideoxynucleosides / Q000494:pharmacology*; D006678:HIV / Q000187:drug effects* / Q000502:physiology; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D014779:Virus Replication / Q000187:drug effects; D016047:Zalcitabine; D015215:Zidovudine / Q000494:pharmacology
D000998:Antiviral Agents; D015224:Dideoxynucleosides; C057503:carbovir; D015215:Zidovudine; D016047:Zalcitabine