NDLI: Novel N-2-(Furyl)-2-(chlorobenzyloxyimino) Ethyl Piperazinyl Quinolones: Synthesis, Cytotoxic Evaluation and Structure-Activity Relationship.

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Novel N-2-(Furyl)-2-(chlorobenzyloxyimino) Ethyl Piperazinyl Quinolones: Synthesis, Cytotoxic Evaluation and Structure-Activity Relationship.

Content Provider	Europe PMC
Author	Mohammadhosseini, Negar Pordeli, Mahboobeh Safavi, Maliheh Firoozpour, Loghman Amin, Fatame Kabudanian Ardestani, Sussan Edraki, Najmeh Shafiee, Abbas Foroumadi, Alireza
Abstract	Quinolone antibacterials are one of the most important classes of pharmacological agents known as potent inhibitors of bacterial DNA gyrase and topoisomerase IV that efficiently inhibit DNA replication and transcription by generating several double-stranded DNA break. Some quinolone derivatives demonstrated inhibitory potential against eukaryote topoismarase II and substantial dose-dependent cytotoxic potential against some cancerous cells. In present study, synthesis and cytotoxic activity evaluation of new series of N-pipearzinyl quinolones containing N-2-(furyl-2 or 3-yl)-2-(chlorobenzyloxyimino) ethyl moiety 7a-i have been studied. Reaction of quinolone, with 2-bromo-1-(furan-2 or 3-yl)ethanone-O-substituted chlorobenzyloxime in DMF in presence of NaHCO3 at room temperature, gave the title compounds N-2-(furan-2 or 3-yl)-2-(chlorobenzyloxyiminoethyl) quinolone 7a-i. Synthesized compounds were further evaluated in-vitro against three human breast tumor cell lines. Preliminary screening indicated that compound 7 g demonstrated significant growth inhibitory potential against all evaluated cell lines. The results of structure-activity relationship study exhibited that quinolone derivatives are superior in cytotoxic potential compared to 1, 8-naphthyridone series. Furthermore, ethyl quinolone derivatives were more potent cytotoxic agents comparing with cyclopropyl quinolones.
ISSN	17350328
Journal	Iranian Journal of Pharmaceutical Research : IJPR
Volume Number	14
PubMed Central reference number	PMC4673937
Issue Number	4
PubMed reference number	26664376
e-ISSN	17266890
Language	English
Publisher	Shaheed Beheshti University of Medical Sciences
Publisher Date	2015-01-01
Publisher Place	Tehran, Iran
Access Restriction	Open
Rights License	This is an Open Access article distributed under the terms of the Creative Commons Attribution License, (http://creativecommons.org/licenses/by/3.0/) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. © 2015 by School of Pharmacy, Shaheed Beheshti University of Medical Sciences and Health Services
Subject Keyword	Furyl N-pipearzinyl quinolones Cytotoxic activity Structure-activity Relationship
Content Type	Text
Resource Type	Article
Subject	Pharmacology, Toxicology and Pharmaceutics Pharmacology (medical)

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