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Potent and selective inhibition of human immunodeficiency virus (HIV)-1 and HIV-2 replication by a class of bicyclams interacting with a viral uncoating event.

Authors
  • De Clercq, E
  • Yamamoto, N
  • Pauwels, R
  • Baba, M
  • Schols, D
  • Nakashima, H
  • Balzarini, J
  • Debyser, Z
  • Murrer, B A
  • Schwartz, D
Type
Published Article
Journal
Proceedings of the National Academy of Sciences of the United States of America
Publication Date
Jun 15, 1992
Volume
89
Issue
12
Pages
5286–5290
Identifiers
PMID: 1608936
Source
Medline
License
Unknown

Abstract

A series of bicyclams have been shown to be potent and selective inhibitors of human immunodeficiency virus (HIV). The compounds are inhibitory to the replication of various HIV-1 and HIV-2 strains in various human T-cell systems, including peripheral blood lymphocytes, at 0.14-1.4 microM, without being toxic to the host cells at 2.2 mM. The bicyclam JM2763 is active against 3'-azido-3'-deoxythymidine (zidovudine; AZT)-resistant HIV-1 strains and acts additively with AZT. Mechanism of action studies revealed that the bicyclams (i.e., JM2763) interact with an early event of the retrovirus replicative cycle, which could be tentatively identified as a viral uncoating event.

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