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Compound for activating latent human immunodeficiency virus, and application thereof in AIDS treatment

A technology for HIV and latent infection, applied in antiviral agents, medical preparations containing active ingredients, organic chemistry, etc., can solve problems such as not achieving expected significant effects

Active Publication Date: 2017-12-26
INST PASTEUR OF SHANGHAI CHINESE ACADEMY OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Multiple HIV-1 latency activating compounds such as the epigenetic modification inhibitor SAHA (aka Vorinostat) have shown promising effects at the cellular level, but clinical trials have not achieved the expected significant effects

Method used

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  • Compound for activating latent human immunodeficiency virus, and application thereof in AIDS treatment
  • Compound for activating latent human immunodeficiency virus, and application thereof in AIDS treatment
  • Compound for activating latent human immunodeficiency virus, and application thereof in AIDS treatment

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0095] FICZ activates Jurkat CD4 in HIV-1 latent infection + T cells

[0096] CD4 of HIV-1 Latent Infection in Human Peripheral Blood + The number of T cells is too low, CD4 per million + One latently infected cell can be isolated from T cells, which increases the difficulty of HIV-1 latent infection research. Currently, research on the molecular mechanism of HIV-1 latent infection and the development of treatment methods mainly use the cell model of latent infection.

[0097] Utilization of HIV-1 Latently Infected Jurkat CD4 + T cells, the compound FICZ was found to significantly activate HIV-1 latency, EC 50 up to 47nM, while the control drug SAHA EC 50 It was 700nM, compared with SAHA, the compound FICZ showed nearly 15-fold activation activity ( figure 2 ). The results show that the compound FICZ activates Jurkat CD4 in HIV-1 latent infection + T cells.

Embodiment 2

[0099] FICZ versus Jurkat CD4 + T cells show lower cytotoxicity

[0100] To test the cytotoxicity of FICZ, different concentrations of FICZ were mixed with HIV-1 latently infected Jurkat CD4 + T cells were co-cultured for 48 hours, and cell survival was detected by MTT method. It was found that FICZ has low cytotoxicity, and when the concentration of FICZ is as high as 50 μM, the cells still maintain a cell viability rate as high as 82%.

Embodiment 3

[0102] FICZ activates HIV-1 in resting infected CD4 + Replication in T cells

[0103] In order to verify the activation effect of FICZ on HIV-1 latent infection, HIV-1 infected patients who had been treated with antiretroviral drugs for more than 5 years and whose viral load could not be detected in plasma were recruited, and the peripheral blood resting infected CD4 + T cells. Treatment of quiescently infected CD4 with the compound FICZ + After 48 hours of T cells, RNA was collected, and HIV-1 replication was detected by quantifying the level of HIV-1 gag mRNA. FICZ (100nM) treatment enhanced the replication of HIV-1, CD4 isolated from 4 infected persons + In T cells, the enhancement factors were 2.6-60 times ( Figure 4 ). The results show that FICZ activates HIV-1 in resting infected CD4 + Replication in T cells.

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PUM

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Abstract

The invention provides an human immunodeficiency virus latent activator and an application thereof, and concretely provides a compound of formula I, or a pharmaceutically acceptable salt thereof. The compound has an excellent activating effect on a latent human immunodeficiency virus. The invention also provides a medicinal composition containing the compound of formula I, and an application thereof in the activation of the latent human immunodeficiency virus.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, and more specifically relates to a compound for activating latently infected AIDS virus and its application in AIDS treatment. Background technique [0002] Since the first case of AIDS was discovered in the United States in 1981, AIDS has spread rapidly around the world. According to UNAIDS statistics, 39 million people worldwide have died of AIDS. As of the end of 2014, approximately 36.9 million people worldwide were living with HIV. Sub-Saharan Africa accounted for the highest proportion of total infections at approximately 71%, followed by Asia and the Pacific at approximately 14%. [0003] Currently, there is still a lack of effective drugs to cure HIV infection worldwide. The goals of treatment at this stage are: to maximize and sustainably reduce the viral load; to obtain immune function reconstruction and maintenance of immune function; to improve the quality of life; to reduce HIV-...

Claims

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Application Information

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IPC IPC(8): A61K31/407A61P31/18C07D487/04
CPCA61K31/407C07D487/04
Inventor 王建华孙丽蒋金凤
Owner INST PASTEUR OF SHANGHAI CHINESE ACADEMY OF SCI
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