Synthesis, Modelling, and Antimitotic Properties of Tricyclic Systems Characterised by a 2-(5-Phenyl-1H-pyrrol-3-yl)-1,3,4-oxadiazole Moiety

Interesting antitumor activity was observed in a series of tricyclic compounds characterized by the presence of a 2-(1H-pyrrol-3-yl)-1,3,4-oxadiazole moiety variously substituted. Their synthesis and their antiproliferative activity on a panel of human tumor cell lines is described. The most interesting compounds 1c and 4c were selected for further evaluation in order to understand their possible mechanism of action. Analysis of cell cycle, tubulin polymerization, modulation of mitotic markers of M phase and apoptosis showed that the antimitotic activity is the primary mechanism of their cytotoxic effects. The experiment performed on isolated tubulin confirm that the compounds act by inducing tubulin polymerization, like taxanes. The binding model against tubulin was also examined by molecular modeling and docking. The results point out that the proposed binding model is able to explain the oxadiazole derivatives activity on the basis of their docking energ

Diamo qualità alla vita: completamento dell'offerta di medicina del dolore e Cure Palliative pediatriche specialistiche in Regione Liguria

il poster dal titolo " Diamo qualità alla vita: completamento dell'offerta di medicina del dolore e Cure Palliative pediatriche specialistiche in Regione Liguria" illustra i risultati ottenuti nella Regione Liguria in materia di cure palliative pediatriche rispetto al quale si colloca la propria attività di consulenza tecnico-scientifica per la realizzazione dell’hospice pediatrico condotta in ambito multidisciplinare attraverso l’accordo tra la Fondazione Maruzza Lefebvre d’Ovidio Onlus e l’Istituto Gaslini

Asymmetric Synthesis of Unsaturated Monocyclic and Bicyclic Nitrogen Heterocycles

Hydrolysis of scalemic trichloroacetamides Cl3CCONHCH(R)CHCH2 and allylation, or acylation with but-3-enoic acid, followed by ring-closing metathesis resulted in the formation of unsaturated pyrrolidine and piperidine building blocks. These were employed in the synthesis of (S)-coniine (R = Pr) and a formal synthesis of (+)-anisomycin (R = p-MeOC6H4). Extension of this methodology with R = CH2CHCH2 employing two ring-closing metatheses resulted in the synthesis of unsaturated quinolizidinone and indolizidinone frameworks