Semi-Automatic Synthesis, Antiproliferative Activity and DNA-Binding Properties of New Netropsin and bis-Netropsin Analogues

Abstract

A general route for the semi-automatic synthesis of some new potential minor groove binders was established. Six four-numbered sub-libraries of new netropsin and bis-netropsin analogues have been synthesized using a Syncore Reactor. The structures of the all new substances prepared in this investigation were fully characterized by NMR (1H, 13C), HPLC and LC-MS. The antiproliferative activity of the obtained compounds was tested on MCF-7 breast cancer cells. The ethidium displacement assay using pBR322 confirmed the DNA-binding properties of the new analogues of netropsin and bis-netropsin.

Keywords

• combinatorial chemistry
• solid phase synthesis
• netropsin analogue
• non-intercalative DNA binding agent
• DNA minor groove binder