41201-58-5Relevant articles and documents
Synthesis of rigid trichostatin A analogs as HDAC inhibitors
Charrier, Cedric,Bertrand, Philippe,Gesson, Jean-Pierre,Roche, Joelle
, p. 5339 - 5344 (2006)
New inhibitors of histone deacetylase (HDAC) have been synthesized and evaluated for their activity toward non small lung cancer cell line H661. Their design is based on indanone (or tetralone) systems leading to trichostatin A (TSA) analogs with limited conformational mobility. Molecular modelization at the AM1 level revealed that the conformations of indane-based analogs and TSA bound to HDAC like protein are similar. The synthesis of these new analogs was achieved by alkylation of an appropriate indanone (or tetralone) to introduce the side chain bearing a terminal ester group, the latter being a precursor of hydroxamic acid and aminobenzamide derivatives. Hydroxamic acids with the TSA side chain were found to be the most active compounds and the presence of the dimethylamino group on the phenyl ring turned out to be essential to achieve low micromolar activities against H661 cancer cells.
Extending the Substrate Scope in the Hydrogenation of Unfunctionalized Tetrasubstituted Olefins with Ir-P Stereogenic Aminophosphine-Oxazoline Catalysts
Biosca, Maria,Salomó, Ernest,De La Cruz-Sánchez, Pol,Riera, Antoni,Verdaguer, Xavier,Pàmies, Oscar,Diéguez, Montserrat
supporting information, p. 807 - 811 (2019/01/26)
Air-stable and readily available Ir-catalyst precursors modified with MaxPHOX-type ligands have been successfully applied in the challenging asymmetric hydrogenation of tetrasubstituted olefins under mild reaction conditions. Gratifyingly, these catalyst precursors are able to efficiently hydrogenate not only a range of indene derivatives (ee's up to 96%) but also 1,2-dihydronapthalene derivatives and acyclic olefins (ee's up to 99%), which both constitute the most challenging substrates for this transformation.
COMPOUNDS, COMPOSITIONS AND METHODS OF TREATING CANCER
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, (2017/07/06)
Disclosed are compounds of formulas I and II, in which R, R0, R1-R4, R7-R10, n, X, Y, Y', and E are as described herein, pharmaceutical compositions containing such compounds. The compounds and pharmaceutical compositions are for use in treating or preventing diseases, for example, cancer.