One drug for two targets: Biological evaluation of antiretroviral agents endowed with antiproliferative activity
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Other documents of the author: Botta, Lorenzo; Maccari, Giorgio; Calandro, Pierpaolo; Tiberi, Marika; Brai, Annalaura; Zamperini, Claudio; Canducci, Filippo; Chiariello, Mario; Martí-Centelles, Rosa; Falomir, Eva; Carda, Miguel
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Show full item recordcomunitat-uji-handle:10234/9
comunitat-uji-handle2:10234/7053
comunitat-uji-handle3:10234/8639
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https://doi.org/10.1016/j.bmcl.2017.03.097 |
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Title
One drug for two targets: Biological evaluation of antiretroviral agents endowed with antiproliferative activityAuthor (s)
Date
2017-06-01Publisher
ElsevierISSN
0960-894XBibliographic citation
BOTTA, Lorenzo, et al. One drug for two targets: Biological evaluation of antiretroviral agents endowed with antiproliferative activity. Bioorganic & Medicinal Chemistry Letters, 2017, vol. 27, no 11, p. 2502-2505.Type
info:eu-repo/semantics/articlePublisher version
http://www.sciencedirect.com/science/article/pii/S0960894X17303621Version
info:eu-repo/semantics/publishedVersionSubject
Abstract
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, ... [+]
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 the possibility to screen a small library of compounds synthesized in our laboratory against opportunistic tumors mainly due to HIV infection like Burkitt’s Lymphoma. From cellular assays and gene expression analysis we identified two promising compounds. These derivatives have the dual action required inhibiting HIV replication in human TZM-bl cells infected with HIV-1 NL4.3 and showing cytotoxic activity on human colon HT-29 and breast adenocarcinoma MCF-7 cells. In addition, preclinical in vitro adsorption, distribution, metabolism, and excretion studies highlighted a satisfactory pharmacokinetic profile. [-]
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Bioorganic & Medicinal Chemistry Letters, 2017, vol. 27, no 11, p. 2502-2505.Investigation project
Ministerio de Economia y Competitividad / CTQ2014-52949-P; Universitat Jaume I / PI-1B2015-75; University Jaume I / E-2013-09Rights
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