Literature DB >> 25799376

Structure-based hybridization, synthesis and biological evaluation of novel tetracyclic heterocyclic azathioxanthone analogues as potential antitumor agents.

Tsung-Chih Chen1, Chia-Lun Wu2, Chia-Chung Lee1, Chun-Liang Chen1, Dah-Shyong Yu3, Hsu-Shan Huang4.   

Abstract

A series of tetracyclic heterocyclic azathioxanthones were synthesized and evaluated for cell proliferations, topoisomerase inhibitions, and NCI-60 cell panel assay, respectively. Compounds 5, 7, 8, 16, and 19 were selected for topoisomerase assay after MTT assay. 7 not only showed cytotoxic effect (IC50 = 2.84 ± 0.64 μM) in PC-3 cells but also revealed topoisomerases inhibition with IC50 (10-25 μM) and increased apoptotic cleavage of PARP and caspase 3 activity. The overall of novel azathioxanthones with different cytostatic and cytotoxic activities should be further developed as new potential candidates for anticancer drugs.
Copyright © 2015 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  Azathioxanthones; Cytostatic and cytotoxic activities; MTT assay; NCI-60 human tumor cell lines; Topoisomerase assays

Mesh：

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Year:  2014        PMID： 25799376     DOI： 10.1016/j.ejmech.2014.09.050

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN： 0223-5234            Impact factor:   6.514


  10 in total

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  10 in total

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