一种具有嵌入特性的新型双噻唑衍生物。
A new bithiazole derivative with intercalative properties.
作者信息
Houssin R, Helbecque N, Bernier J L, Henichart J P
机构信息
INSERM U16, Lille, France.
出版信息
J Biomol Struct Dyn. 1986 Oct;4(2):219-29. doi: 10.1080/07391102.1986.10506341.
In the course of studies related to new molecules with intercalative properties, we have been led to design and synthesize a bithiazole derivative, namely the 2-phenyl-6-[2'-(4'-(ethoxy-carbonyl)thiazolyl)]thiazolo[3,2- b][1,2,4]triazole (PETT). Its interaction with calf thymus DNA was studied using thermal denaturation and viscometry. Our results set in evidence that PETT acts as an intercalator, giving delta Tm, elongation and unwinding of DNA comparable to the values obtained for daunorubicin. The discrepancy between the data presented herein and those precedently obtained for bleomycin and bleomycin models provide evidence that these bithiazole derivatives interact differently with DNA.
在与具有嵌入性质的新分子相关的研究过程中，我们着手设计并合成了一种双噻唑衍生物，即2-苯基-6-[2'-(4'-(乙氧羰基)噻唑基)]噻唑并[3,2-b][1,2,4]三唑（PETT）。使用热变性和粘度测定法研究了它与小牛胸腺DNA的相互作用。我们的结果表明，PETT起到嵌入剂的作用，其使DNA的ΔTm、伸长和解旋与柔红霉素所获得的值相当。本文所呈现的数据与先前针对博来霉素和博来霉素模型所获得的数据之间的差异证明，这些双噻唑衍生物与DNA的相互作用不同。
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