One drug for two targets: Biological evaluation of antiretroviral agents endowed with antiproliferative activity
Impacto
Scholar |
Otros documentos de la autoría: Botta, Lorenzo; Maccari, Giorgio; Calandro, Pierpaolo; Tiberi, Marika; Brai, Annalaura; Zamperini, Claudio; Canducci, Filippo; Chiariello, Mario; Martí-Centelles, Rosa; Falomir, Eva; Carda, Miguel
Metadatos
Mostrar el registro completo del ítemcomunitat-uji-handle:10234/9
comunitat-uji-handle2:10234/7053
comunitat-uji-handle3:10234/8639
comunitat-uji-handle4:
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https://doi.org/10.1016/j.bmcl.2017.03.097 |
Metadatos
Título
One drug for two targets: Biological evaluation of antiretroviral agents endowed with antiproliferative activityAutoría
Fecha de publicación
2017-06-01Editor
ElsevierISSN
0960-894XCita bibliográfica
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.Tipo de documento
info:eu-repo/semantics/articleVersión de la editorial
http://www.sciencedirect.com/science/article/pii/S0960894X17303621Versión
info:eu-repo/semantics/publishedVersionPalabras clave / Materias
Resumen
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. [-]
Publicado en
Bioorganic & Medicinal Chemistry Letters, 2017, vol. 27, no 11, p. 2502-2505.Proyecto de investigación
Ministerio de Economia y Competitividad / CTQ2014-52949-P; Universitat Jaume I / PI-1B2015-75; University Jaume I / E-2013-09Derechos de acceso
Copyright © Elsevier B.V.
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