Ricerc@Sapienza

This thesis explores the applications of organocatalysis and its combination with metal catalysis for the enantioselective synthesis of novel oxygen- and nitrogen-containing heterocycles. The developed procedures rely on both covalent- and hydrogen-bounding organocatalysis and metal coordination catalysis. The first project focused on the development of an efficient asymmetric synthesis of new 4-amino-isochromanones starting from anilines and 2-formylbenzoates.

Rhinovirus (RV)?, member of the Enterovirus genus, is known to be involved in more than half of the common colds. Through advances in mol. biol., rhinoviruses have also been assocd. with exacerbations of chronic pulmonary diseases (e.g., asthma, chronic obstructive pulmonary disease (COPD) and cystic fibrosis)?. In the current investigation, the authors develop a novel series of 4,?5-?dimethoxybenzyl derivs. that potently inhibits rhinovirus replication. Compd.

Microtubules are an attractive target for the development of active anti-leukemia agents (1). Despite some evidence, the therapeutic potential of colchicine site binding agents in chronic myeloid leukemia (CML) has not been adequately explored.
Recently, starting from previously reported aroylindoles (ARIs, e.g. 1) we have developed 3-aroyl-1-arylpyrroles (ARAPs, e.g. 2) via benzocracking approach (Chart 1) (2). Pursuing our studies, we designed and synthesized 3-aroyl-1,4-diarylpyrroles (ARDAPs, 3-16) as potential anticancer agents (3).