Design and synthesis of dual activated bioprobe for proteins and DNAs

我们使用稠环丁醇作为通过环收缩重排激活的前体，开发了对pH敏感的DNA裂解剂。设计稳定阳离子中间体的分子对提高反应活性具有重要意义。此外，我们还发现苯并稠环丁醇具有切割DNA的活性，并且这种活性随着浓度的升高和pH值的升高而增强。我们实验室正在对DNA烷基化机理和活性更高的化合物进行进一步的研究。

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.