Ricerc@Sapienza

A series of benzo[b]thiophen-3-ols were synthesised and investigated as potential human monoamine oxidase (hMAO) inhibitors in vitro as well as ex vivo in rat cortex synaptosomes by means of evaluation of 3,4-dihydroxyphenylacetic acid/dopamine (DOPAC/DA) ratio and lactate dehydrogenase (LDH) activity. Most of these compounds possessed high selectivity for the MAO-B isoform and a discrete antioxidant and chelating potential.

Gliomas are malignant brain tumors characterized by rapid spread and growth into neighboring tissues and graded I-IV by theWorld Health Organization. Glioblastoma is the fastest growing and most devastating IV glioma. The aim of this paper is to evaluate the biological effects of two potent and selective Monoamine Oxidase B (MAO-B) inhibitors, Cmp3 and Cmp5, in C6 glioma cells and in CTX/TNA2 astrocytes in terms of cell proliferation, apoptosis occurrence, inflammatory events and cell migration. These compounds decrease C6 glioma cells viability sparing normal astrocytes.

In the last years the continuous efforts in the development of novel and effective inhibitors of human
monoamine oxidases (hMAOs) promoted the discovery of new agents able to effectively and selectively
bound one of the two isoforms (hMAO-A and hMAO-B). However, the parent chalcone scaffold still
covers an important role in hMAOs inhibition. In the present work, we focused our attention on the
researches performed in the last five years, involving chalcones or compounds that can be correlated to