The DOI matches its Crossref record; 3 of the 3 references it cites were found in a registry or an index.
Styrylquinoline Derivatives: A New Class of Potent HIV-1 Integrase Inhibitors That Block HIV-1 Replication in CEM Cells
Open accessAbstract
On the basis of the fact that several polynucleotidyl transferases, related to HIV integrase, contain in their active site two divalent metal cations, separated by ca. 4 A, new potential HIV integrase inhibitors were designed, in which a quinoline substructure is linked to an aryl nucleus possessing various hydroxy substitution patterns, by means of an ethylenic spacer. Although the most active compounds contain the catechol structure, this group is not essential for the activity, since compound 21 that lacks such a moiety is a potent drug, implicating the presence of a different pharmacophore. The most promising styrylquinolines thus synthesized inhibit HIV-1 integrase in vitro at micromolar or submicromolar concentrations and block HIV replication in CEM cells, with no significant cellular toxicity in a 5-day period assay. These inhibitors are active against integrase core domain-mediated disintegration, suggesting that fragment 50-212 is their actual target. These new styrylquinolines may provide lead compounds for the development of novel antiretroviral agents for AIDS therapeutics, based upon inhibition of HIV integrase. They might also be used in the elucidation of the mechanism of inhibition of this enzyme; e.g., they could serve as candidates for cocrystallization studies with HIV integrase.
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Dyda, F., Hickman, A. B., Jenkins, T. M., Engelman, A., Craigie, R., & Davies, D. R. (1994) · Science · doi:10.1126/science.7801124 · Cited by 810
Crystal structure of the ribonuclease H domain of HIV-1 reverse transcriptase
Davies, J. F., Hostomska, Z., Hostomsky, Z., Jordan, S. R., & Matthews, D. A. (1991) · Science · doi:10.1126/science.1707186 · Cited by 570
Three-dimensional structure of ribonuclease H from E. coli
Katayanagi, K., Miyagawa, M., Matsushima, M., Ishikawa, M., Kanaya, S., Ikehara, M., Matsuzaki, T., & Morikawa, K. (1990) · Nature · doi:10.1038/347306a0 · Cited by 349
Cited by
Integrase inhibitors to treat HIV/Aids
Pommier, Y., Johnson, A. A., & Marchand, C. (2005) · Nature Reviews Drug Discovery · doi:10.1038/nrd1660 · Cited by 688
Developing a Dynamic Pharmacophore Model for HIV-1 Integrase
Carlson, H. A., Masukawa, K. M., Rubins, K., Bushman, F. D., Jorgensen, W. L., Lins, R. D., Briggs, J. M., & McCammon, J. A. (2000) · Journal of Medicinal Chemistry · doi:10.1021/jm990322h · Cited by 259
Rabaaoui, S., Zouhiri, F., Lançon, A., Leh, H., d'Angelo, J., & Wattel, E. (2008) · Antimicrobial Agents and Chemotherapy · doi:10.1128/aac.01361-07 · Cited by 23
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Metadata
- Authors
- Mekouar, K., Mouscadet, J.-F., Desmaële, D., Subra, F., Leh, H., Savouré, D., Auclair, C., & d'Angelo, J.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 1998-06-25
- Volume
- 41
- Issue
- 15
- Pages
- 2846-2857
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2067663373
- Cited by
- 222
- References
- 3
- FWCI
- 5.03
- Type
- journal article
- Language
- en
- Open access
- green
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- Mekouar, K., Mouscadet, J.-F., Desmaële, D., Subra, F., Leh, H., Savouré, D., Auclair, C., & d'Angelo, J. (1998). Styrylquinoline Derivatives: A New Class of Potent HIV-1 Integrase Inhibitors That Block HIV-1 Replication in CEM Cells. Journal of Medicinal Chemistry. https://doi.org/10.1021/jm980043e
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