Madurahydroxylactone Derivatives as Dual Inhibitors of Human Immunodeficiency Virus Type 1 Integrase and RNase H
2007 ◽
Vol 52
(1)
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pp. 361-364
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Keyword(s):
Rnase H
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ABSTRACT A series of 29 madurahydroxylactone derivatives was evaluated for dual inhibition of human immunodeficiency virus type 1 (HIV-1) integrase and RNase H. While most of the compounds exhibited similar potencies for both enzymes, two of the derivatives showed 10- to 100-fold-higher selectivity for each enzyme, suggesting that distinct pharmacophore models could be generated. This study exemplifies the common and divergent structural requirements for the inhibition of two structurally related HIV-1 enzymes and demonstrates the importance of systematically screening for both integrase and RNase H when developing novel inhibitors.
2003 ◽
Vol 77
(8)
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pp. 4710-4721
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2012 ◽
Vol 56
(5)
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pp. 2581-2589
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2003 ◽
Vol 77
(20)
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pp. 11150-11157
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1997 ◽
Vol 8
(4)
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pp. 353-362
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Interaction between Human Immunodeficiency Virus Type 1 Reverse Transcriptase and Integrase Proteins
2004 ◽
Vol 78
(10)
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pp. 5056-5067
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2011 ◽
Vol 18
(22)
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pp. 3335-3342
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2004 ◽
Vol 78
(16)
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pp. 8761-8770
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2000 ◽
Vol 74
(20)
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pp. 9668-9679
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