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Title 

Design, synthesis and biological evaluation of 1,3-diphenylbenzo[f][1,7]naphthyrdines

Authors 

S K ArepalliB ParkK LeeH JoK Y JunY KwonJong Soon KangJ K JungH Lee

Publisher 

Elsevier

Issue Date 

2017

Citation 

Bioorganic & Medicinal Chemistry

Keywords 

1,3-Diphenylbenzo[f][1,7]benzonaphthyrdinesCytotoxic agentsHuman Topoisomerase IIα inhibitorsImino Diels-Alder reactionMolecular docking studies

Abstract 

A novel series of twenty 1,3-diphenylbenzo[f][1,7]benzonaphthyrdine derivatives were designed and synthesized through intermolecular imino Diels-Alder reaction. Their in vitro cytotoxic activities were evaluated against six human cancer cell lines (NCIH23, HCT15, NUGC-3, ACHN, PC-3, and MDA-MB-231). Majority of synthesized compounds exhibited significant cytotoxic activities against all tested human cancer cell lines. Among them 4l, 4m, and 4o derivatives exhibited most promising cytotoxic activities. Furthermore these compounds were evaluated against human Topoisomerase IIα inhibition. Interestingly, the compound 4l exhibited 1.3 and 1.2 times more potent human Topoisomerase IIα inhibition than the reference drug etoposide in both 100 ?M and 20 ?M concentrations respectively. Molecular docking studies for the compound 4l have also been executed by Sybyl X-2.1 in which it reveals the binding site of the compound 4l with topo IIα DNA cleavage site where etoposide was situated. The benzo[f][1,7]naphthyridine ring was stacked between the DNA bases of the cleavage site

ISSN 

0968-0896

Link 

http://dx.doi.org/10.1016/j.bmc.2017.08.030

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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