Inhibition of Human Immunodeficiency Virus Type 1 Integration by Diketo Derivatives
2002 ◽
Vol 46
(10)
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pp. 3292-3297
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Keyword(s):
ABSTRACT A series of diketo derivatives was found to inhibit human immunodeficiency virus type 1 (HIV-1) integrase activity. Only L-708,906 inhibited the replication of HIV-1(IIIB) (50% effective concentration, 12 μM), HIV-1 clinical strains, HIV-1 strains resistant to reverse transcriptase or fusion inhibitors, HIV-2 (ROD strain) and simian immunodeficiency virus (MAC251). The combinations of L-708,906 with zidovudine, nevirapine, or nelfinavir proved to be subsynergistic. In cell culture, addition of L-708,906 could be postponed for 7 h after infection, a moment coinciding with HIV integration. Inhibition of integration in cell culture was confirmed by quantitative Alu-PCR.
2004 ◽
Vol 48
(11)
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pp. 4349-4359
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2016 ◽
Vol 71
(5-6)
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pp. 105-109
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2005 ◽
Vol 49
(6)
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pp. 2314-2321
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2001 ◽
Vol 45
(9)
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pp. 2510-2516
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