Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)

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Chemical Compound Review:

CHEMBL414850 5-(1,1-dioxothiazinan-2-yl)- N-[(4...

Synonyms: AG-F-45965, SureCN1198641, AC1L9XHC, CTK1D6669, L-870810, ...

Jin, H. et al., Hazuda, D.J. et al., Dayam, R. et al.

Jin, Cai, Schacherer, Jabri, Tsiang, Fardis, Chen, Chen, Kim, Hazuda, Anthony, Gomez, Jolly, Wai, Zhuang, Fisher, Embrey, Guare, Egbertson, Vacca, Huff, Felock, Witmer, Stillmock, Danovich, Grobler, Miller, Espeseth, Jin, Chen, Lin, Kassahun, Ellis, Wong, Xu, Pearson, Schleif, Cortese, Emini, Summa, Holloway, Young,

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Disease relevance of L-870810

We describe here the identification and characterization of L-870,810, a small-molecule inhibitor of HIV-1 integrase with potent antiviral activity in cell culture and good pharmacokinetic properties [1].
A novel class of tri-cyclic HIV integrase inhibitors were designed based on conformational analysis of 1,6-naphthyridine carboxamide compound L-870810 and docking the designed inhibitor into the active site of our integrase enzyme model [2].

High impact information on L-870810

S-1360 (1) and L-870,810 (2) are examples of beta-diketo acid related compounds to enter clinical trials [3].

References

A naphthyridine carboxamide provides evidence for discordant resistance between mechanistically identical inhibitors of HIV-1 integrase. Hazuda, D.J., Anthony, N.J., Gomez, R.P., Jolly, S.M., Wai, J.S., Zhuang, L., Fisher, T.E., Embrey, M., Guare, J.P., Egbertson, M.S., Vacca, J.P., Huff, J.R., Felock, P.J., Witmer, M.V., Stillmock, K.A., Danovich, R., Grobler, J., Miller, M.D., Espeseth, A.S., Jin, L., Chen, I.W., Lin, J.H., Kassahun, K., Ellis, J.D., Wong, B.K., Xu, W., Pearson, P.G., Schleif, W.A., Cortese, R., Emini, E., Summa, V., Holloway, M.K., Young, S.D. Proc. Natl. Acad. Sci. U.S.A. (2004) [Pubmed]
Design, synthesis, and SAR studies of novel and highly active tri-cyclic HIV integrase inhibitors. Jin, H., Cai, R.Z., Schacherer, L., Jabri, S., Tsiang, M., Fardis, M., Chen, X., Chen, J.M., Kim, C.U. Bioorg. Med. Chem. Lett. (2006) [Pubmed]
Diketo acid pharmacophore. 2. Discovery of structurally diverse inhibitors of HIV-1 integrase. Dayam, R., Sanchez, T., Neamati, N. J. Med. Chem. (2005) [Pubmed]

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