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2 results on '"ANDREA MILELLI"'

1. Design, Synthesis, and Biological Evaluation of Substituted Naphthalene Imides and Diimides as Anticancer Agent∞.

Author

Vincenzo Tumiatti, Andrea Milelli, Anna Minarini, Marialuisa Micco, Anna Gasperi Campani, Laura Roncuzzi, Daniela Baiocchi, Jessica Marinello, Giovanni Capranico, Maddalena Zini, Claudio Stefanelli, and Carlo Melchiorre

Subjects
*DRUG design, *ORGANIC synthesis, *NAPHTHALENE, *IMIDES, *ANTINEOPLASTIC agents, *CARBOXYLIC acids, *CELL-mediated cytotoxicity, *P53 protein, *THERAPEUTICS
Abstract

Naphthalimmide (NI) and 1,4,5,8-naphthalentetracarboxylic diimide (NDI) derivatives were synthesized and evaluated for their antiproliferative activity. NDI derivatives 1−9were more cytotoxic than the corresponding NI derivatives 10−18. The molecular mechanisms of 1and 2were investigated in comparison to mitonafide. They interacted with DNA, were not topoisomerase IIα poisons, triggered caspase activation, caused p53 protein accumulation, and down-regulated AKT survival. Furthermore, 1and 2caused a decrease of ERK1/2 and, unlike mitonafide, inhibited ERKs phosphorylation. [ABSTRACT FROM AUTHOR]

Published
2009
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2. Structure−Activity Relationships of Acetylcholinesterase Noncovalent Inhibitors Based on a Polyamine Backbone. 4. Further Investigation on the Inner Spacer.

Author

Vincenzo Tumiatti, Andrea Milelli, Anna Minarini, Michela Rosini, Maria Laura Bolognesi, Marialuisa Micco, Vincenza Andrisano, Manuela Bartolini, Francesca Mancini, Maurizio Recanatini, Andrea Cavalli, and Carlo Melchiorre

Subjects
*ACETYLCHOLINESTERASE, *ENZYME inhibitors, *POLYAMINES, *LIGANDS (Biochemistry), *AMYLOID beta-protein, *ALZHEIMER'S disease
Abstract

Novel multi-target-directed ligands were designed by replacing the inner dipiperidino function of 3with less flexible or completely rigid moieties to obtain compounds endowed with multiple biological properties that might be relevant to Alzheimer’s disease. 15was the most interesting, inhibiting AChE in the nanomolar range and inhibiting AChE-induced and self-promoted β-amyloid aggregation in the micromolar range. [ABSTRACT FROM AUTHOR]

Published
2008
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