0000000001054924
AUTHOR
Barreca M.
Identification of pyrrolo[3',4':3,4]cyclohepta[1,2-d][1,2]oxazoles as promising new candidates for the treatment of lymphomas
Unsatisfactory outcomes for relapsed/refractory lymphoma patients prompt continuing efforts to develop new therapeutic strategies. Our previous studies on pyrrole-based anti-lymphoma agents led us to synthesize a new series of twenty-six pyrrolo[3′,4':3,4]cyclohepta[1,2-d] [1,2]oxazole derivatives and study their antiproliferative effects against a panel of four non-Hodgkin lymphoma cell lines. Several candidates showed significant anti-proliferative effects, with IC50's reaching the sub-micromolar range in at least one cell line, with compound 3z demonstrating sub-micromolar growth inhibitory effects towards the entire panel. The VL51 cell line was the most sensitive, with an IC50 value of…
Osservazioni su alcuni parametri di composizione e igienico-sanitari del latte d’asina
Sono riportati i risultati di un’indagine sulla qualità del latte d’asina prelevato presso quattro aziende siciliane da 27 animali nel corso della lattazione. La ricerca approfondisce alcuni aspetti relativi alla composizione ed all’assetto igienico-sanitario del prodotto, anche in funzione di quanto esplicitato nel Regolamento (CE) 853/2004 che include “altre specie” lattifere e sottolinea la futura emanazione di una normativa più specifica sulla qualità del latte e dei derivati. Gli AA auspicano che la presente indagine, unitamente ad altri studi sull’argomento, fornisca un contributo al fondamento scientifico sul quale dovrebbe essere basata la formulazione di specifici criteri normativi…
Novel tricyclic pyrrolo-quinolines as pharmacological correctors of the mutant CFTR chloride channel
AbstractF508del, the most frequent mutation in cystic fibrosis (CF), impairs the stability and folding of the CFTR chloride channel, thus resulting in intracellular retention and CFTR degradation. The F508del defect can be targeted with pharmacological correctors, such as VX-809 and VX-445, that stabilize CFTR and improve its trafficking to plasma membrane. Using a functional test to evaluate a panel of chemical compounds, we have identified tricyclic pyrrolo-quinolines as novel F508del correctors with high efficacy on primary airway epithelial cells from CF patients. The most effective compound, PP028, showed synergy when combined with VX-809 and VX-661 but not with VX-445. By testing the …