Facile synthesis of a polyether-tethered dimeric berberine as a highly effective DNA-cleaving agent in the presence of Cu(ii) ion

MedChemComm
2013.0

Abstract

A polyether-tethered dimeric berberine was synthesized and found to be capable of efficiently converting pBR322 DNA into open circular and linear forms in the presence of Cu(II) ions under physiological conditions, most probably via an oxidative mechanism. Michaelis–Menten analysis afforded ca. 3.5 × 10⁹ -fold rate acceleration over uncatalyzed cleavage of supercoiled DNA. The probable mode of action is also briefly discussed.

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