Literature DB >> 24094433

Design, synthesis and antiproliferative evaluation of fluorenone analogs with DNA topoisomerase I inhibitory properties.

Chia-Chung Lee1, Deh-Ming Chang, Kuo-Feng Huang, Chun-Liang Chen, Tsung-Chih Chen, Yang Lo, Jih-Hwa Guh, Hsu-Shan Huang.   

Abstract

A series of 2,7-diamidofluorenones were designed, synthesized, and screened by SRB assay. Some synthesized compounds exhibited antitumor activities in submicromolar range. Ten compounds (3a, 3b, 3c, 3g, 3j, 3l, 4a, 4h, 4i, and 4j) were also selected by NCI screening system and 3c (GI50=1.66 μM) appeared to be the most active agent of this series. Furthermore, 3c attenuated topoisomerase I-mediated DNA relaxation at low micromolar concentrations. These results indicated that fluorenones have potential to be further developed into anticancer drugs. Crown
Copyright © 2013. Published by Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Fluorenones; NCI 60-cell panel assay; Tilorone; Topoisomerase I

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Substances：

Year:  2013        PMID： 24094433     DOI： 10.1016/j.bmc.2013.09.006

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN： 0968-0896            Impact factor:   3.641


  3 in total

1.  Discovery, synthesis and structure-activity analysis of symmetrical 2,7-disubstituted fluorenones as urea transporter inhibitors.

Authors:  Sujin Lee; Cristina Esteva-Font; Puay-Wah Phuan; Marc O Anderson; A S Verkman
Journal:  Medchemcomm       Date:  2015       Impact factor: 3.597

2.  Extraction, preliminary characterization and evaluation of in vitro antitumor and antioxidant activities of polysaccharides from Mentha piperita.

Authors:  Xin Liu; Zhen-Liang Sun; Ai-Rong Jia; Ya-Ping Shi; Rui-Hong Li; Pei-Ming Yang
Journal:  Int J Mol Sci       Date:  2014-09-15       Impact factor: 5.923

3.  New O-Aryl-Carbamoyl-Oxymino-Fluorene Derivatives with MI-Crobicidal and Antibiofilm Activity Enhanced by Combination with Iron Oxide Nanoparticles.

Authors:  Ilinca Margareta Vlad; Diana Camelia Nuță; Robert Viorel Ancuceanu; Miron Teodor Caproiou; Florea Dumitrascu; Ioana Cristina Marinas; Mariana Carmen Chifiriuc; Luminita Gabriela Măruţescu; Irina Zarafu; Ioana Raluca Papacocea; Bogdan Ștefan Vasile; Adrian Ionuț Nicoară; Cornelia-Ioana Ilie; Anton Ficai; Carmen Limban
Journal:  Molecules       Date:  2021-05-18       Impact factor: 4.411
  3 in total

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