Synthesis and Biological Investigation of 1,2,4-Triazolo[4,3-a]azines as Potential HSF1 Inductors
作者:Irina A. Utepova、Polina O. Serebrennikova、Oleg N. Chupakhin、Irina V. Guzhova、Elena R. Mikhaylova、Andrey P. Antonchick
DOI:10.1055/s-0040-1719907
日期:2022.6
4-triazines containing heterocyclic and metallocene fragments were obtained by one-pot oxidative cyclization of heterocyclic hydrazones in the presence of hypervalent iodine(III) reagents. For 1,2,4-triazolo[4,3-a]azines, the ability to activate HSF1 was investigated. The obtained compounds were shown to increase the degree of HSF1 activation. It was shown that the 1,2,4-triazines can be used to induce
在高价碘 (III) 试剂存在下,通过杂环腙的一锅氧化环化获得含有杂环和茂金属片段的稠合 1,2,4-三嗪衍生物。对于 1,2,4-三唑并[4,3- a ]嗪,研究了激活 HSF1 的能力。所得化合物显示可增加 HSF1 活化程度。结果表明,1,2,4-三嗪可用于诱导 Hsp70 表达并降低突变 HTT 聚集体形成的程度。