5-Ethynylarylnaphthalimides as antitumor agents: Synthesis and biological evaluation

Quintana-Espinoza Patricia; Martin-Acosta Pedro; Amesty AngelMartin-Rodriguez PatriciaLorenzo-Castrillejo IsabelFernandez-Perez LeandroMachin FelixEstevez-Braun Ana

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5-Ethynylarylnaphthalimides as antitumor agents: Synthesis and biological evaluation

机译：5-Ethynylarylnaphthalimides as antitumor agents: Synthesis and biological evaluation

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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. (C) 2017 Elsevier Ltd. All rights reserved.

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来源
《Bioorganic and medicinal chemistry》 |2017年第6期|1976-1983|共8页
作者
Quintana-Espinoza Patricia; Martin-Acosta Pedro; Amesty AngelMartin-Rodriguez PatriciaLorenzo-Castrillejo IsabelFernandez-Perez LeandroMachin FelixEstevez-Braun Ana;
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作者单位

Univ La Laguna, Inst Univ Bio Organ Antonio Gonzalez CIBICAN, Dept Quim Organ, Avda Astrofis Fco;

Univ Las Palmas Gran Canaria, Inst Univ Invest Biomed Sanitarias IUIBS, Dept Ciencias Clin;

Hosp Univ Nuestra Seriora Candelaria, Unidad Invest, Carretera Rosario 145, Santa Cruz de Tenerife;

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原文格式 PDF
正文语种英语
中图分类药学;
关键词
Naphthalimides; Antiproliferative activity; Topoisomerase II; DNA damage; Saccaromyces cereviciae;

5-Ethynylarylnaphthalimides as antitumor agents: Synthesis and biological evaluation

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