1202920-72-6Relevant articles and documents
Exploring in vitro and in vivo Hsp90 inhibitors activity against human protozoan parasites
Giannini, Giuseppe,Battistuzzi, Gianfranco
supporting information, p. 462 - 465 (2015/01/30)
A set of compounds, previously selected as potent Hsp90α inhibitors, has been studied on a panel of human parasites. 5-Aryl-3,4-isoxazolediamide derivatives (1) were active against two protozoa, Trypanosoma brucei rhodesiense and Plasmodium falciparum, with a good tolerability toward cytotoxicity on non-malignant L6 rat myoblast cell line, unlike the 1,5-diaryl,4-carboxamides-1,2,3-triazole derivatives (2) which, while showing a single-digit nM range activity against the same protozoa, were also highly cytotoxic on L6 cells. In a subsequent in vivo study, two isoxazolediamide derivatives, 1a and 1b, were very efficacious on the sleeping sickness-causing agent with a clear parasitaemia during treatment. These data, however, showed that not all protozoa are sensitive to Hsp90 inhibitors, as well as not all Hsp90 inhibitors are equally active on parasites.
5-PHENYL-ISOXAZOLE-3-CARBOXAMIDES MODULATING HSP90 WITH ANTITUMORAL ACTIVITIES
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Page/Page column 37; 38, (2010/04/03)
The present invention relates to formula I compounds having antitumoural activities through, as one possible biological target, the molecular chaperone heat shock protein 90 (Hsp90) inhibition. The invention includes the use of such compounds in medicine,