TY - JOUR
T1 - DNA targeted platinum complexes
T2 - Synthesis, cytotoxicity and DNA interactions of cis-dichloroplatinum(II) complexes tethered to phenazine-1- carboxamides
AU - Perrin, Leah C.
AU - Prenzler, Paul D.
AU - Cullinane, Carleen
AU - Phillips, Don R.
AU - Denny, William A.
AU - McFadyen, W. David
PY - 2000/7/15
Y1 - 2000/7/15
N2 - A series of intercalator-tethered platinum(II) complexes PtLCl2 have been prepared, where L are the diamine ligands N-[2- [(aminoethyl)amino]ethyl]-phenazine-1-carboxamide, N-[3-[(2- aminoethyl)amino]propyl]-phenazine-1-carboxamide, N-[4-[(2- aminoethyl)amino]butyl]-phenazine-1-carboxamide and N-[5- [(aminoethyl)amino]pentyl]-phenazine-1-carboxamide. Measurements of the time- course of unwinding of supercoiled pUC19 plasmid DNA by the phenazine complexes PtLCl2 reveal that the presence of the intercalator leads to enhanced rates of DNA platination when compared with the complex Pt(en)Cl2. The platinum(II) complexes where the polymethylene linker chain contains three, four or five carbon atoms are considerably more cytotoxic against murine P388/W than either cisplatin, Pt(en)Cl2, or the metal-free ligands themselves. (C) 2000 Elsevier Science S.A.
AB - A series of intercalator-tethered platinum(II) complexes PtLCl2 have been prepared, where L are the diamine ligands N-[2- [(aminoethyl)amino]ethyl]-phenazine-1-carboxamide, N-[3-[(2- aminoethyl)amino]propyl]-phenazine-1-carboxamide, N-[4-[(2- aminoethyl)amino]butyl]-phenazine-1-carboxamide and N-[5- [(aminoethyl)amino]pentyl]-phenazine-1-carboxamide. Measurements of the time- course of unwinding of supercoiled pUC19 plasmid DNA by the phenazine complexes PtLCl2 reveal that the presence of the intercalator leads to enhanced rates of DNA platination when compared with the complex Pt(en)Cl2. The platinum(II) complexes where the polymethylene linker chain contains three, four or five carbon atoms are considerably more cytotoxic against murine P388/W than either cisplatin, Pt(en)Cl2, or the metal-free ligands themselves. (C) 2000 Elsevier Science S.A.
KW - Cis-Dichloroplatinum (II)
KW - Cytotoxicity
KW - DNA
KW - Phenazine-1-carboxamides
KW - Unwinding
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U2 - 10.1016/S0162-0134(00)00092-1
DO - 10.1016/S0162-0134(00)00092-1
M3 - Article
C2 - 11001439
AN - SCOPUS:0034661015
VL - 81
SP - 111
EP - 117
JO - Bioinorganic Chemistry
JF - Bioinorganic Chemistry
SN - 0162-0134
IS - 1-2
ER -