Department of Chemistry, Indian Institute of Technology, Kharagpur 721 302, India.
Bioorg Med Chem Lett. 2010 Nov 15;20(22):6831-5. doi: 10.1016/j.bmcl.2010.08.085. Epub 2010 Sep 23.
C(2)-symmetric azobenzene-amino acid linked bis(propargyl sulfones) 1 and 2 containing stable E azo moiety have been synthesized. Upon irradiation with long wavelength UV these compounds isomerized to the Z-form, whose thermal reisomerization to the E-isomer slowed down considerably Under basic pH, the compounds showed DNA cleavage in μmolar concentrations with the Z-isomers showing better cleaving efficiency. The difference in cleaving efficiency between the Z and the E-isomer is more than the corresponding pair of sulfones without amino acid linker.
C(2)-对称偶氮苯-氨基酸连接的双(炔丙基砜)1 和 2 含有稳定的 E 偶氮部分，已被合成。这些化合物在长波长紫外光照射下异构化为 Z 型，其热异构化为 E-型的速度大大减慢。在碱性 pH 下，这些化合物在微摩尔浓度下表现出 DNA 断裂，其中 Z 异构体具有更好的断裂效率。Z 异构体和 E-异构体之间的断裂效率差异大于没有氨基酸连接体的相应砜对。
