TY - JOUR
T1 - Design, synthesis, and biological evaluation of substituted naphthalene imides and diimides as anticancer agent∞
AU - Tumiatti, Vincenzo
AU - Milelli, Andrea
AU - Minarini, Anna
AU - Micco, Marialuisa
AU - Campani, Anna Gasperi
AU - Roncuzzi, Laura
AU - Baiocchi, Daniela
AU - Marinello, Jessica
AU - Capranico, Giovanni
AU - Zini, Maddalena
AU - Stefanelli, Claudio
AU - Melchiorre, Carlo
PY - 2009/12/10
Y1 - 2009/12/10
N2 - Naphthalimmide (NI) and 1,4,5,8-naphthalentetracarboxylic diimide (NDI) derivatives were synthesized and evaluated for their antiproliferative activity. NDI derivatives 1-9 were more cytotoxic than the corresponding NI derivatives 10-18. The molecular mechanisms of 1 and 2 were investigated in comparison to mitonafide. They interacted with DNA, were not topoisomerase IIR poisons, triggered caspase activation, caused p53 protein accumulation, and down-regulated AKT survival. Furthermore, 1 and 2 caused a decrease of ERK1/2 and, unlike mitonafide, inhibited ERKs phosphorylation. ∞ Dedicated to Professor Fulvio Gualtieri on the occasion of his retirement.
AB - Naphthalimmide (NI) and 1,4,5,8-naphthalentetracarboxylic diimide (NDI) derivatives were synthesized and evaluated for their antiproliferative activity. NDI derivatives 1-9 were more cytotoxic than the corresponding NI derivatives 10-18. The molecular mechanisms of 1 and 2 were investigated in comparison to mitonafide. They interacted with DNA, were not topoisomerase IIR poisons, triggered caspase activation, caused p53 protein accumulation, and down-regulated AKT survival. Furthermore, 1 and 2 caused a decrease of ERK1/2 and, unlike mitonafide, inhibited ERKs phosphorylation. ∞ Dedicated to Professor Fulvio Gualtieri on the occasion of his retirement.
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U2 - 10.1021/jm901131m
DO - 10.1021/jm901131m
M3 - Article
C2 - 19954251
AN - SCOPUS:72249110438
VL - 52
SP - 7873
EP - 7877
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
SN - 0022-2623
IS - 23
ER -