Synergetic DNA‐Cleaving Activities of the Metal Complexes of a Polyether‐Tethered Pyrrole‐polyamide Dimer |
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Authors: | Chun‐Qiong Zhou Yan‐Ling Lin Jin‐Xiang Chen Wen‐Hua Chen |
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Institution: | School of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, P.?R. China, (fax: +86‐20‐61648533) |
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Abstract: | A simple polyether‐tethered pyrrole‐polyamide dimer 1 was synthesized in 50% yield from the reaction of 2,2,2‐trichloro‐1‐(1‐methyl‐4‐nitro‐1H‐pyrrol‐2‐yl)ethanone with 2,2′‐1,2‐ethanediylbis(oxy)]bisethanamine, and fully characterized on the basis of 1H‐ and 13C‐NMR, MS, HR‐MS, and IR data. Agarose gel‐electrophoresis study of the cleavage of plasmid pBR322 DNA by the complexes of compound 1 with seven metal ions indicated that most of the metal complexes were capable of efficiently cleaving DNA at pH 7.0 and 37°. Among them, the CuII complex exhibited the highest activity, with the maximal catalytic rate constant kmax and Michaelis constant KM being 5.61 h?1 and 7.30 mM , respectively. Spectroscopic, ESI‐MS, ethidium‐bromide (EB) displacement, and viscosity experiments indicated that compound 1 could form a 1 : 1 complex with CuII ion, and that this complex showed moderate binding affinity toward calf‐thymus DNA. |
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Keywords: | Pyrrole?polyamide dimers Copper complexes DNA |
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