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补骨脂素的3-氨基和3-氧基衍生物:制备及其与DNA的相互作用。

3-Amino- and 3-oxy-derivatives of psoralen: preparation and interactions with DNA.

作者信息

Antonello C, Marciani Magno S, Gia O, Baessato O, Palumbo M

出版信息

Farmaco Sci. 1981 Jul;36(7):565-84. doi: 10.1002/chin.198144193.

Abstract

3-Amino- and 3-oxy-derivatives of psoralen, thus having electron-donating groups at the 3-position of the alpha-pyronic ring, were prepared and studied as regards their capacities of interaction and photoreaction with native DNA in vitro. Very interesting properties were shown especially by the 3-amino-derivatives, namely 3-amino-4'-methylpsoralen and 3-diethylaminoacetylamido-4'-methylpsoralen, having a very high photobinding capacity with DNA and behaving as pure, or fairly pure, monofunctional reagents. These properties appear to be quite suitable for the therapeutic treatment of psoriasis and other skin diseases characterized by an increased reproducing activity of epidermal cells.

摘要

补骨脂素的3-氨基和3-氧基衍生物,即在α-吡喃酮环的3位具有供电子基团,已被制备并研究了它们在体外与天然DNA相互作用和光反应的能力。特别是3-氨基衍生物,即3-氨基-4'-甲基补骨脂素和3-二乙氨基乙酰氨基-4'-甲基补骨脂素,表现出非常有趣的性质,它们与DNA具有非常高的光结合能力,并且表现为纯的或相当纯的单功能试剂。这些性质似乎非常适合治疗银屑病和其他以表皮细胞增殖活性增加为特征的皮肤病。

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