Role of Metalation in the Topoisomerase IIα inhibition and antiproliferation activity of a series of α-heterocyclic-N 4-substituted thiosemicarbazones and their Cu(II) complexes Journal Article

   

Authors:	Zeglis, B. M.; Divilov, V.; Lewis, J. S.
Article Title:	Role of Metalation in the Topoisomerase IIα inhibition and antiproliferation activity of a series of α-heterocyclic-N 4-substituted thiosemicarbazones and their Cu(II) complexes
Abstract:	The topoisomerase-IIα inhibition and antiproliferative activity of α-heterocyclic thiosemicarbazones and their corresponding copper(II) complexes have been investigated. The CuII(thiosemicarbazonato)Cl complexes were shown to catalytically inhibit topoisomerase-IIα at concentrations (0.3-7.2 μM) over an order of magnitude lower than their corresponding thiosemicarbazone ligands alone. The copper complexes were also shown to inhibit the proliferation of breast cancer cells expressing high levels of topoisomerase-IIα (SK-BR-3) at lower concentrations than cells expressing lower levels of the enzyme (MCF-7). © 2011 American Chemical Society.
Keywords:	controlled study; protein expression; unclassified drug; human cell; doxorubicin; antineoplastic agent; cell proliferation; biological marker; enzyme inhibition; breast cancer; etoposide; structure activity relation; dna; drug mechanism; cell culture; cancer cell; dna topoisomerase inhibitor; ic 50; cell strain mcf 7; heterocyclic compound; thiosemicarbazone derivative; copper complex; metallation; cell strain; 2 formylpyridine n4 allylthiosemicarbazonatochlorocopper; 2 formylpyridine n4 benzylthiosemicarbazonatochlorocopper; 2 formylpyridine n4 pyrrolidinylthiosemicarbazonatochlorocopper; copper derivative; dna topoisomerase (atp hydrolysing) a; merbarone; cell strain sk br 3
Journal Title:	Journal of Medicinal Chemistry
Volume:	54
Issue:	7
ISSN:	0022-2623
Publisher:	American Chemical Society
Date Published:	2011-04-14
Start Page:	2391
End Page:	2398
Language:	English
DOI:	10.1021/jm101532u
PROVIDER:	scopus
PUBMED:	21391686
PMCID:	PMC4151564
DOI/URL:	http://www.scopus.com/inward/record.url?eid=2-s2.0-79953771126&partnerID=40&md5=8f8e1a35990acb0bd162b60bd81abe01
Notes:	--- - "Export Date: 23 June 2011" - "CODEN: JMCMA" - "Source: Scopus"

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