Please use this identifier to cite or link to this item: http://hdl.handle.net/10553/35747
Title: 5-Ethynylarylnaphthalimides as antitumor agents: synthesis and biological evaluation
Authors: Quintana-Espinoza, Patricia
Martín-Acosta, Pedro
Amesty, Ángel
Martín Rodríguez, Patricia 
Lorenzo-Castrillejo, Isabel
Fernández Pérez, Leandro Fco 
Machín, Félix
Estévez-Braun, Ana
UNESCO Clasification: 32 Ciencias médicas
Keywords: Naphthalimides
Antiproliferative activity
Topoisomerase II
DNA damage
Saccaromyces cereviciae
Issue Date: 2017
Project: "Evaluación Preclinica de Nuevas Estructuras Quimicas Diseñadas Para Inhibir la Ruta Oncogenica Jak-Stat O Como Moduladores Selectivos de Los Receptores Estrógenos" 
Desarrollo Preclínico de Nuevas Estructuras Bioactivas Moduladoras de Las Actividades Oncogénicas de Stat3/5 O de Los Receptores de Estrógenos 
Journal: Bioorganic and Medicinal Chemistry 
Abstract: A set of 5-ethynylarylnaphthalimides was synthesized by Sonogashira cross-coupling reactions and evaluated for antiproliferative and antitopoisomerase II in vitro activities. Furthermore docking studies of these molecules as DNA-intercalators were carried out and the in vivo DNA-damaging activity was also determined with the model organism Saccharomyces cerevisiae. From the obtained results three naphthalimides 6, 13 and 14 showed strong topoisomerase II inhibitory activity. These three molecules also presented good docking scores as DNA-intercalators using a self-complementary oligodeoxynucleotide d (ATGCAT)(2) as a model, and compounds 13 and 14 were among the most cytotoxic in the in vivo DNA-damaging activity.
URI: http://hdl.handle.net/10553/35747
ISSN: 0968-0896
DOI: 10.1016/j.bmc.2017.02.024
Source: Bioorganic and Medicinal Chemistry[ISSN 0968-0896],v. 25, p. 1976-1983
Appears in Collections:Artículos
Show full item record

SCOPUSTM   
Citations

6
checked on Sep 12, 2021

WEB OF SCIENCETM
Citations

6
checked on Sep 12, 2021

Page view(s)

71
checked on Sep 5, 2021

Google ScholarTM

Check

Altmetric


Share



Export metadata



Items in accedaCRIS are protected by copyright, with all rights reserved, unless otherwise indicated.