[The anti-HIV-1 activities of benzophenones non-nucleoside reverse transcriptase inhibitors in vitro].
Yao Xue Xue Bao
; 51(11): 1704-10, 2016 11.
Article
en Zh
| MEDLINE
| ID: mdl-29908113
To evaluate the anti-HIV-1 activities of 5 benzophenones non-nucleoside reverse transcriptase inhibitors (NNRTIs) such as DY1203, DY1204, DY1119, DY1208 and DY1209 in vitro, the cytotoxicity of 5 compounds were tested on C8166, MT-4, H9 and PBMC with the MTT assay. The anti-HIV-1 activities of compounds were evaluated on laboratory-adapted strain, drug-resistant strains and primary isolated strains by p24 antigen expression ELISA. The inhibition of HIV-1 recombinant reverse transcriptase activity was assessed by ELISA assay. Among 5 compounds, DY1203 and DY1204 showed low cytotoxicities with CC(50) greater than 200 µg·m L(-1). DY1119, DY1208 and DY1209 showed strong anti-HIV-1 activities against HIV-1(IIIB,) HIV-1(74V,) HIV-1(RF/V82F/184V,) HIV-1(NL4-3) (gp41(36G)N42S,) HIV-1(KM018,) HIV-1(TC-1) and HIV-1(Wan.) However, NNRTIs drug-resistant strain HIV-1(A17) showed different resistance to these compounds. The 5 compounds proved active against HIV-1 recombinant reverse transcriptase. DY1208 is expected to become a new lead compound for its high therapeutic index. The results can provide new information for HIV-1 drug research and promote the development of new HIV-1 drugs.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Benzofenonas
/
Inhibidores de la Transcriptasa Inversa
/
Fármacos Anti-VIH
Límite:
Humans
Idioma:
Zh
Revista:
Yao Xue Xue Bao
Año:
2016
Tipo del documento:
Article
Pais de publicación:
China