One drug for two targets: Biological evaluation of antiretroviral agents endowed with antiproliferative activity
作者： Lorenzo Botta , Giorgio Maccari , Pierpaolo Calandro , Marika Tiberi , Annalaura Brai
DOI: 10.1016/J.BMCL.2017.03.097
关键词:
摘要: AIDS-related cancer diseases are malignancies with low incidence on healthy people that affect mostly subjects already immunocompromised. The connection between HIV/AIDS and these cancers has not been established yet, but a weakened immune system is certainly the main cause. We envisaged possibility to screen small library of compounds synthesized in our laboratory against opportunistic tumors mainly due HIV infection like Burkitt’s Lymphoma. From cellular assays gene expression analysis we identified two promising compounds. These derivatives have dual action required inhibiting replication human TZM-bl cells infected HIV-1 NL4.3 showing cytotoxic activity colon HT-29 breast adenocarcinoma MCF-7 cells. In addition, preclinical vitro adsorption, distribution, metabolism, excretion studies highlighted satisfactory pharmacokinetic profile.
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