Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 12, Issue 24, Pages 6383-6387Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2004.09.038
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Funding
- NIAID NIH HHS [AI-33066] Funding Source: Medline
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Two thia-DCK analogs (3a,b) were synthesized and evaluated for inhibition of HIV-1 replication in H9 lymphocytes. Compound 3a showed potent anti-HIV activity with an EC50 value of 0.14 muM and a therapeutic index of 1110. However, the corresponding 6-tert-butyl-substituted compound (3b) showed no suppression. The bioassay results indicated that thia-DCK analogs merit attention as potential HIV-1 inhibitors. (C) 2004 Elsevier Ltd. All rights reserved.
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