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Basic Quinolinonyl Diketo Acid Derivatives as Inhibitors of HIV Integrase and their Activity against RNase H Function of Reverse Transcriptase
[Image: see text] A series of antiviral basic quinolinonyl diketo acid derivatives were developed as inhibitors of HIV-1 IN. Compounds 12d,f,i inhibited HIV-1 IN with IC(50) values below 100 nM for strand transfer and showed a 2 order of magnitude selectivity over 3′-processing. These strand transfe...
| Autores principales: | , , , , , , , , , , , , , , , , , , , |
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| Formato: | Online Artículo Texto |
| Lenguaje: | English |
| Publicado: |
American Chemical
Society
2014
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| Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4203401/ https://www.ncbi.nlm.nih.gov/pubmed/24684270 http://dx.doi.org/10.1021/jm5001503 |
| _version_ | 1782340396811026432 |
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| author | Costi, Roberta Métifiot, Mathieu Chung, Suhman Cuzzucoli Crucitti, Giuliana Maddali, Kasthuraiah Pescatori, Luca Messore, Antonella Madia, Valentina Noemi Pupo, Giovanni Scipione, Luigi Tortorella, Silvano Di Leva, Francesco Saverio Cosconati, Sandro Marinelli, Luciana Novellino, Ettore Le Grice, Stuart F. J. Corona, Angela Pommier, Yves Marchand, Christophe Di Santo, Roberto |
| author_facet | Costi, Roberta Métifiot, Mathieu Chung, Suhman Cuzzucoli Crucitti, Giuliana Maddali, Kasthuraiah Pescatori, Luca Messore, Antonella Madia, Valentina Noemi Pupo, Giovanni Scipione, Luigi Tortorella, Silvano Di Leva, Francesco Saverio Cosconati, Sandro Marinelli, Luciana Novellino, Ettore Le Grice, Stuart F. J. Corona, Angela Pommier, Yves Marchand, Christophe Di Santo, Roberto |
| author_sort | Costi, Roberta |
| collection | PubMed |
| description | [Image: see text] A series of antiviral basic quinolinonyl diketo acid derivatives were developed as inhibitors of HIV-1 IN. Compounds 12d,f,i inhibited HIV-1 IN with IC(50) values below 100 nM for strand transfer and showed a 2 order of magnitude selectivity over 3′-processing. These strand transfer selective inhibitors also inhibited HIV-1 RNase H with low micromolar potencies. Molecular modeling studies based on both the HIV-1 IN and RNase H catalytic core domains provided new structural insights for the future development of these compounds as dual HIV-1 IN and RNase H inhibitors. |
| format | Online Article Text |
| id | pubmed-4203401 |
| institution | National Center for Biotechnology Information |
| language | English |
| publishDate | 2014 |
| publisher | American Chemical
Society |
| record_format | MEDLINE/PubMed |
| spelling | pubmed-42034012015-03-31 Basic Quinolinonyl Diketo Acid Derivatives as Inhibitors of HIV Integrase and their Activity against RNase H Function of Reverse Transcriptase Costi, Roberta Métifiot, Mathieu Chung, Suhman Cuzzucoli Crucitti, Giuliana Maddali, Kasthuraiah Pescatori, Luca Messore, Antonella Madia, Valentina Noemi Pupo, Giovanni Scipione, Luigi Tortorella, Silvano Di Leva, Francesco Saverio Cosconati, Sandro Marinelli, Luciana Novellino, Ettore Le Grice, Stuart F. J. Corona, Angela Pommier, Yves Marchand, Christophe Di Santo, Roberto J Med Chem [Image: see text] A series of antiviral basic quinolinonyl diketo acid derivatives were developed as inhibitors of HIV-1 IN. Compounds 12d,f,i inhibited HIV-1 IN with IC(50) values below 100 nM for strand transfer and showed a 2 order of magnitude selectivity over 3′-processing. These strand transfer selective inhibitors also inhibited HIV-1 RNase H with low micromolar potencies. Molecular modeling studies based on both the HIV-1 IN and RNase H catalytic core domains provided new structural insights for the future development of these compounds as dual HIV-1 IN and RNase H inhibitors. American Chemical Society 2014-03-31 2014-04-24 /pmc/articles/PMC4203401/ /pubmed/24684270 http://dx.doi.org/10.1021/jm5001503 Text en Copyright © 2014 American Chemical Society Terms of Use (http://pubs.acs.org/page/policy/authorchoice_termsofuse.html) |
| spellingShingle | Costi, Roberta Métifiot, Mathieu Chung, Suhman Cuzzucoli Crucitti, Giuliana Maddali, Kasthuraiah Pescatori, Luca Messore, Antonella Madia, Valentina Noemi Pupo, Giovanni Scipione, Luigi Tortorella, Silvano Di Leva, Francesco Saverio Cosconati, Sandro Marinelli, Luciana Novellino, Ettore Le Grice, Stuart F. J. Corona, Angela Pommier, Yves Marchand, Christophe Di Santo, Roberto Basic Quinolinonyl Diketo Acid Derivatives as Inhibitors of HIV Integrase and their Activity against RNase H Function of Reverse Transcriptase |
| title | Basic Quinolinonyl Diketo
Acid Derivatives as Inhibitors
of HIV Integrase and
their Activity against RNase H Function of Reverse Transcriptase |
| title_full | Basic Quinolinonyl Diketo
Acid Derivatives as Inhibitors
of HIV Integrase and
their Activity against RNase H Function of Reverse Transcriptase |
| title_fullStr | Basic Quinolinonyl Diketo
Acid Derivatives as Inhibitors
of HIV Integrase and
their Activity against RNase H Function of Reverse Transcriptase |
| title_full_unstemmed | Basic Quinolinonyl Diketo
Acid Derivatives as Inhibitors
of HIV Integrase and
their Activity against RNase H Function of Reverse Transcriptase |
| title_short | Basic Quinolinonyl Diketo
Acid Derivatives as Inhibitors
of HIV Integrase and
their Activity against RNase H Function of Reverse Transcriptase |
| title_sort | basic quinolinonyl diketo
acid derivatives as inhibitors
of hiv integrase and
their activity against rnase h function of reverse transcriptase |
| url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4203401/ https://www.ncbi.nlm.nih.gov/pubmed/24684270 http://dx.doi.org/10.1021/jm5001503 |
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