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Photoactivated DNA cleavage and anticancer activity of pyrenyl-terpyridine lanthanide complexes

  作者 Hussain, A; Gadadhar, S; Goswami, TK; Karande, AA; Chakravarty, AR  
  选自 期刊  European Journal of Medicinal Chemistry;  卷期  2012年50-1;  页码  319-331  
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[摘要]Lanthanide(III) complexes [Ln(R-tpy)(acac)(NO(3))(2)] (Ln = La(III) in 1, 2; Gd(III) in 4, 5) and [Ln(py-tpy)(sacac)(NO(3))(2)] (Ln = La(III), Gd(III), 6), where R-tpy is 4'-phenyl-2,2':6',2 ''-terpyridine (ph-tpy in 1, 4), 4'-(1-pyrenyl)-2,2':6',2 ''-terpyridine (py-tpy in 2, 3, 5 and 6), acac is acetylacetonate and sacac is 4-hydroxy-6-{4-[(beta-D-glucopyranoside)oxy]phenyl}hex-3,5-dien-2-onate, were prepared to study their DNA photocleavage activity and photocytotoxicity. Complexes [La(ph-tpy)(acac)(E-tOH)(NO(3))(2)] (1a) and [Gd(ph-tpy)(acac)(NO(3))(2)] (4) were characterized by X-ray crystallography. The 1:1 electrolytic complexes bind to calf thymus DNA. The py-tpy complexes cleave pUC19 DNA and exhibit remarkable photocytotoxicity in HeLa cells in UV-A light of 365 nm with apoptotic cell death (IC(50): similar to 40 nM in light, >200 mu M in dark). Confocal microscopy using HeLa cells reveal primarily cytosolic localization of the complexes. (C) 2012 Elsevier Masson SAS. All rights reserved.

 
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