The synthesis and antitumor activity in normoxic and hypoxic conditions of a series of pyrazolo[5, 1-c][1,2,4]benzotriazine and its related analogues are reported. All compounds were tested on human colorectal adenocarcinoma cell line HCT-8 and for compounds 15 and 20, which show to have selective cytotoxicity in hypoxic and in normoxic conditions respectively, ROS production, cell cycle, and DNA fragmentation were measured. This preliminary study encouraged us to consider 15 and 20 as interesting leads for further optimization.

Synthesis of new pyrazolo[5,1-c][1,2,4]benzotriazines, pyrazolo[5,1-c]pyrido[4,3-e][1,2,4]triazines and their open analogues as cytotoxic agents in normoxic and hypoxic conditions / G. Ciciani; M. Coronnello; G. Guerrini; S.Selleri; M.Cantore; P. Failli; E. Mini; A. Costanzo. - In: BIOORGANIC & MEDICINAL CHEMISTRY. - ISSN 1464-3391. - ELETTRONICO. - 16:(2008), pp. 9409-9419. [10.1016/j.bmc.2008.09.055]

Synthesis of new pyrazolo[5,1-c][1,2,4]benzotriazines, pyrazolo[5,1-c]pyrido[4,3-e][1,2,4]triazines and their open analogues as cytotoxic agents in normoxic and hypoxic conditions.

CICIANI, GIOVANNA;CORONNELLO, MARCELLA MARIA;GUERRINI, GABRIELLA;SELLERI, SILVIA;FAILLI, PAOLA;MINI, ENRICO;COSTANZO, ANNARELLA
2008

Abstract

The synthesis and antitumor activity in normoxic and hypoxic conditions of a series of pyrazolo[5, 1-c][1,2,4]benzotriazine and its related analogues are reported. All compounds were tested on human colorectal adenocarcinoma cell line HCT-8 and for compounds 15 and 20, which show to have selective cytotoxicity in hypoxic and in normoxic conditions respectively, ROS production, cell cycle, and DNA fragmentation were measured. This preliminary study encouraged us to consider 15 and 20 as interesting leads for further optimization.
2008
16
9409
9419
G. Ciciani; M. Coronnello; G. Guerrini; S.Selleri; M.Cantore; P. Failli; E. Mini; A. Costanzo
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Utilizza questo identificatore per citare o creare un link a questa risorsa: https://hdl.handle.net/2158/320997
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