Design and synthesis of dual activated bioprobe for proteins and DNAs

我们已经开发出ph负责的DNA切割剂，使用融合环丁醇作为前体，通过环收缩重排激活。设计分子稳定阳离子中间体对提高反应性具有重要意义。此外，我们还发现，苯并融合环丁醇具有DNA裂解活性，且该活性在浓度越高、pH越酸的条件下越强。我们的实验室正在进一步研究DNA烷基化机理和更高活性的化合物。

We have developed pH-responsible DNA cleaving agents using fused-cyclobutanols as precursors activated via ring contraction rearrangement. It is important for improvement of reactivity to design molecules stabilizing cation intermediates. In addition, we found that benzo-fused cyclobutanol showed DNA cleavage activity and this activity was stronger with higher concentration and more acidic pH condition. Further investigation about DNA alkylation mechanism and higher active compounds are ongoing in our laboratory.