Ricerc@Sapienza

A straightforward one-pot approach to the synthesis of challenging 12-arylindolo[1,2-c]quinazolin-6(5H)-ones is described. Starting from readily available o-(o-aminophenylethynyl)trifluoroacetanilides, palladium-catalyzed aminoarylation of the triple bond with ArI, ArBr, and ArN2 +BF4 – is followed by cyclization of the resulting N-trifluoro­acetyl-2-(o-aminophenyl)-3-aryl indole. This sequential reaction provides the title compounds by means of a rare elimination of trifluoromethane.

Unprecedented hydrolysis reactions are observed in the gas phase in clusters containing doubly-charged vanadium oxides and hydroxide anions, SO2and H2O. The experimental and computational study shows the cooperative effects of the vanadium species, V2O62-and HV3O92-, and sulfur dioxide on the enhancement of the hydrogen bonds of water that allows the acid-base reaction and charge separation in the doubly-charged ion.

A multi-component Povarov reaction was used for the preparation of [4], [5] and [6]aza- and azaoxahetero helical-shaped compounds. The oxidation of the tetrahydroquinolinic primary Povarov adducts to the aromatic quinolines is mandatory to achieve a helical-shaped structure and can be carried out in a one-pot fashion with DDQ. Resolution of [5] and [6]heterohelicenes was successfully performed by chiral HPLC.

DNA is an entity shielded by mechanisms that maintain genomic stability and are essential for living cells; however, DNA is constantly subject to assaults from the environment throughout the cellular life span, making the genome susceptible to mutation and irreparable damage. Cells are prepared to mend such events through cell death as an extrema ratio to solve those threats from a multicellular perspective. However, in cells under various stress conditions, checkpoint mechanisms are activated to allow cells to have enough time to repair the damaged DNA.

c-MET pathway over-activation is the signature of malignancy acquisition or chemotherapy resistance of many cancers. We recently demonstrated that type II Testicular Germ Cell Tumours (TGCTs) express c-MET receptor. In particular, we elucidated that the non-seminoma lesions express c-MET protein at higher level, compared with the seminoma ones. In line with this observation, NTERA-2 clone D1 (NT2D1) non-seminoma cells increase their proliferation, migration and invasion in response to Hepatocyte Growth Factor (HGF).