Results 191 to 200 of about 30,382,849 (226)
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Styrylquinazoline Derivatives as HIV-1 Integrase Inhibitors
Archiv der Pharmazie, 2002Styrylquinazoline derivatives were prepared by Perkin condensation and evaluated for inhibitory activity against HIV-1 integrase. Among them, compound 5c containing a free catechol ring was the most potent (IC(50)=0.8 +/- 1.9 microM)and showed 6-fold more potency than the corresponding styrylquinoline compound (IC(50) = 130.7 +/- 8.6 microM).
Jae Yeol, Lee +4 more
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Hydroxylated Aromatic Inhibitors of HIV-1 Integrase
Journal of Medicinal Chemistry, 1995Efficient replication of HIV-1 requires integration of a DNA copy of the viral genome into a chromosome of the host cell. Integration is catalyzed by the viral integrase, and we have previously reported that phenolic moieties in compounds such as flavones, caffeic acid phenethyl ester (CAPE, 2), and curcumin confer inhibitory activity against HIV-1 ...
Terrence R. Jr. Burke +9 more
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Expression of HIV‐1 integrase in CEM cells inhibits HIV‐1 replication
The Journal of Gene Medicine, 2004AbstractBackgroundHIV‐1 integrase (IN) is an interesting target for the gene therapy of AIDS. Although the in vivo functions are not well characterized, it is thought that IN has pleiotropic effects and plays a central role in the interplay between the virus and the host cell. Expression of IN in mammalian cells has proven difficult. We have previously
Johan, van Griensven +7 more
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Development of an HIV‐1 integrase genotyping assay for HIV‐1 subtype AE
Journal of Medical Virology, 2018An human immunodeficiency virus (HIV)‐1 integrase (IN) genotyping assay was developed to evaluate clinical samples from patients infected with HIV‐1 subtype AE, a subtype highly prevalent in Asia. The HIV‐1 IN gene was amplified from plasma‐derived HIV‐1 viral RNA via reverse transcription polymerase chain reaction followed by population sequencing ...
Yang Liu +3 more
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Eigen Value Analysis of HIV-1 Integrase Inhibitors
Journal of Chemical Information and Computer Sciences, 2001A three-dimensional quantitative structure activity relationship using the eigen value analysis (EVA) paradigm applied to 41 HIV-1 integrase inhibitors that inhibit integrase mediated cleavage (3'-processing step) and integration (3'-strand transfer step) in vitro was performed.
Mahindra T. Makhija, Vithal M. Kulkarni
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HIV‐1 Integrase Inhibitors: Update and Perspectives
2008Publisher Summary The chapter focuses on the recent advances in understanding the cellular mechanisms of human immunodeficiency virus (HIV) integration and the sites of actions of inhibitors. The chapter presents list of the known mutations that have been characterized for HIV‐1 integrase (IN) with their impact on IN activity, viral replication, and ...
Elena A, Semenova +2 more
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HIV-1 Resistance to Integrase Inhibitors
2017Over the past three decades, new antiretroviral drugs have been rapidly developed and expanded for use in the clinic. Antiretroviral therapy (ART) generally combines at least three different drugs for treatment of HIV-infected patients. As more new antiretroviral drugs (ARVs) belonging to different classes have become available, ART has greatly ...
Ying-Shan Han +2 more
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Recent Advances in Small-Molecule HIV-1 Integrase Inhibitors
Current Medicinal Chemistry, 2021Zhe JIN, Chun Hu, Chao Zhang
exaly