Basic quinolinonyl diketo acid derivatives as inhibitors of HIV integrase and their activity against RNase H function of reverse transcriptase.
Basic quinolinonyl diketo acid derivatives as inhibitors of HIV integrase and their activity against RNase H function of reverse transcriptase.
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DOI：
10.1021/jm5001503
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发表时间：
2014-04-24
影响因子：
7.3
通讯作者：
Di Santo R
中科院分区：
文献类型：
--
作者：
Costi R;Métifiot M;Chung S;Cuzzucoli Crucitti G;Maddali K;Pescatori L;Messore A;Madia VN;Pupo G;Scipione L;Tortorella S;Di Leva FS;Cosconati S;Marinelli L;Novellino E;Le Grice SF;Corona A;Pommier Y;Marchand C;Di Santo R
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 IC50 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.
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影响因子：
2.9
作者：
Greenwald, J;Le, V;Choe, S
通讯作者：
Choe, S
DOI：
10.1073/pnas.96.23.13040
发表时间：
1999-11-09
影响因子：
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DOI：
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DOI：
10.1073/pnas.0506924102
发表时间：
2005-11-29
影响因子：
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作者：
Cherepanov, P;Ambrosio, ALB;Engelman, A
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