ArticleBioorganic & medicinal chemistry letters2010
Scaffold rearrangement of dihydroxypyrimidine inhibitors of HIV integrase: Docking model revisited.
Article in Bioorganic & medicinal chemistry letters, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed.
- 4,5-Dihydroxypyrimidine Methyl Carboxylates, Carboxylic Acids, and Carboxamides as Inhibitors of Human Cytomegalovirus pUL89 Endonuclease.Journal of medicinal chemistry · 2022Article
- Discovery and Structure-Activity-Relationship Study of N-Alkyl-5-hydroxypyrimidinone Carboxamides as Novel Antitubercular Agents Targeting Decaprenylphosphoryl-β-d-ribose 2'-Oxidase.Journal of medicinal chemistry · 2018Article
- Can 5-methylcytosine analogues with extended alkyl side chains guide DNA methylation?Chemical communications (Cambridge, England) · 2018Article
- N-Substituted Quinolinonyl Diketo Acid Derivatives as HIV Integrase Strand Transfer Inhibitors and Their Activity against RNase H Function of Reverse Transcriptase.Journal of medicinal chemistry · 2015Article
- Basic quinolinonyl diketo acid derivatives as inhibitors of HIV integrase and their activity against RNase H function of reverse transcriptase.Journal of medicinal chemistry · 2014Article
- Mutations in the amino terminus of herpes simplex virus type 1 gL can reduce cell-cell fusion without affecting gH/gL trafficking.Journal of virology · 2014Article
- 6-Benzoyl-3-hydroxypyrimidine-2,4-diones as dual inhibitors of HIV reverse transcriptase and integrase.Bioorganic & medicinal chemistry letters · 2011Article
- 3-Hydroxypyrimidine-2,4-diones as an inhibitor scaffold of HIV integrase.Journal of medicinal chemistry · 2011Article
- Structural biology of retroviral DNA integration.Virology · 2011Review
- N-3 Hydroxylation of Pyrimidine-2,4-diones Yields Dual Inhibitors of HIV Reverse Transcriptase and Integrase.ACS medicinal chemistry letters · 2011Article
- Molecular mechanisms of retroviral integrase inhibition and the evolution of viral resistance.Proceedings of the National Academy of Sciences of the United States of America · 2010Article
Corrections and comments
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Authors and funding
5 authors.
Funding
Abstract
A series of dihydroxypyrimidine (DHP) derivatives were designed as inhibitors of HIV integrase (IN) based on known homology models. Through chemical synthesis and biochemical assays it was found that the activity profile of these compounds largely deviates from predictions with existing models. With the recently disclosed IN crystal structure of prototype foamy virus (PFV), a new HIV IN homology model was constructed featuring a critical IN/DNA interface previously lacking. With this new model, docking results completely corroborated observed biological activities. This new model should provide a more accurate and improved platform for the design of new inhibitors of HIV IN.
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