|
|||||
|
|
Development of tricyclic hydroxy-1H-pyrrolopyridine-trione containing HIV-1 integrase inhibitors |
|
| Authors: | Zhao Xue Zhi Maddali Kasthuraiah Metifiot Mathieu Smith Steven J Vu B Christie Marchand Christophe Hughes Stephen H Pommier Yves Burke Terrence R |
| Institution: | a Chemical Biology Laboratory, Molecular Discovery Program, Center for Cancer Research, National Cancer Institute-Frederick, National Institutes of Health, Frederick, MD 21702, United States b Laboratory of Molecular Pharmacology, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Bethesda, MD 20892, United States c HIV Drug Resistance Program, Center for Cancer Research, National Cancer Institute-Frederick, National Institutes of Health, Frederick, MD 21702, United States |
| Abstract: | New tricyclic HIV-1 integrase (IN) inhibitors were prepared that combined structural features of bicyclic pyrimidinones with recently disclosed 4,5-dihydroxy-1H-isoindole-1,3(2H)-diones. This combination resulted in the introduction of a nitrogen into the aryl ring and the addition of a fused third ring to our previously described inhibitors. The resulting analogues showed low micromolar inhibitory potency in in vitro HIV-1 integrase assays, with good selectivity for strand transfer relative to 3′-processing. |
| Keywords: | HIV-1 integrase Inhibit Raltegravir Cycloaddition |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ | |