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4‐Picoline‐2,2′:6′,2″‐terpyridine‐platinum(II) — A potent intercalator of DNA
Author(s) -
McCoubrey Angela,
Latham Harriet C.,
Cook Peter R.,
Rodger Alison,
Lowe Gordon
Publication year - 1996
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/0014-5793(95)01537-x
Subject(s) - terpyridine , chemistry , platinum , ethidium bromide , intercalation (chemistry) , picoline , binding constant , circular dichroism , dna , stereochemistry , binding site , crystallography , pyridine , medicinal chemistry , inorganic chemistry , organic chemistry , metal , biochemistry , catalysis
4‐Picoline‐2,2′:6′,2″‐terpyridine‐platinum(II) is shown in a ligation assay to unwind and so intercalate into DNA. Circular dichroism is used to determine an equilibrium binding constant of approximately 2 × 10 7 M −1 for the most stable binding mode of 4‐picoline‐2,2′:6′,2″‐terpyridine‐platinum(II) to poly[d(A‐T) 2 ] with a site size of about 4 base pairs, and about 1 × 10 6 M −1 for a second binding mode with a site size of about 2 base pairs. Fluorescence spectroscopy provides further evidence for the strong equilibrium binding constant of 4‐picoline‐2,2′:6′,2″‐terpyridine‐platinum(II) in that it displaces ethidium bromide bound to DNA. The double positive charge on 4‐picoline‐2,2′:6′,2″‐terpyridine‐platinum(II), together with the intercalative binding mode is probably responsible for the large binding constant.

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