1027915-16-7Relevant articles and documents
IMIDAZO[1,2-A]PYRIDINE DERIVATIVES FOR USE AS INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION
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Page/Page column 51, (2016/03/22)
The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.
Development of chromanes as novel inhibitors of the uncoupling proteins
Rial, Eduardo,Rodriguez-Sanchez, Leonor,Aller, Patricio,Guisado, Arancha,Mar Gonzalez-Barroso,Gallardo-Vara, Eunate,Redondo-Horcajo, Mariano,Castellanos, Esther,Fernandez De La Pradilla, Roberto,Viso, Alma
body text, p. 264 - 274 (2011/10/01)
The uncoupling proteins (UCPs) are mitochondrial carriers that modulate the energetic efficiency and, as a result, can lower superoxide levels. Here, we describe the discovery of a small-molecule inhibitor of the UCPs. Screening of potential UCP1 regulators led to the identification of chromane derivatives that inhibit its proton conductance. Members of the UCP family can act as a defense against oxidative stress and, thus, UCP2 plays a protective role in tumor cells. High UCP2 levels have been associated with chemoresistance. We demonstrate that chromanes also inhibit UCP2 and, in HT-29 human carcinoma cells, cause oxidative stress. The chromane derivatives can act synergistically with chemotherapeutic agents; for instance, they increase the toxicity of arsenic trioxide in HT-29 cells. These findings open a promising line in the development of novel anticancer agents.