Dall'Acqua F, Vedaldi D, Guiotto A, Rodighiero P, Carlassare F, Baccichetti F, Bordin F
J Med Chem. 1981 Jul;24(7):806-11. doi: 10.1021/jm00139a008.
The interactions both in the ground and in the excited state between various methylangelicins, previously prepared with the aim to increase the low photobiological activity of the parent angelicin 1, and DNA have been studied. In general, the new methylangelicins show an increased capacity to photobind monofunctionally to DNA and a parallel increment of photobiological activity in comparison with the parent 1. This increase appears to be connected with various factors, such as the augmented affinity toward DNA for the dark complex formation and the electronic effect connected with the introduction into 1 of one or two methyl groups. The new compounds, on the basis of their photobiological activity and their lack of skin phototoxicity, appear as possible agents for the photochemistry of skin diseases characterized by cell hyperproliferation.
此前为提高母体白芷素1较低的光生物学活性而制备的各种甲基白芷素与DNA在基态和激发态下的相互作用已得到研究。总体而言，与母体1相比，新的甲基白芷素显示出单功能光结合到DNA上的能力增强，以及光生物学活性的相应提高。这种提高似乎与多种因素有关，例如对形成暗复合物的DNA的亲和力增强，以及与在1中引入一个或两个甲基相关的电子效应。基于其光生物学活性和缺乏皮肤光毒性，新化合物似乎是用于以细胞过度增殖为特征的皮肤病光化学治疗的可能药物。
