Department of Organic Chemistry, Latvian Institute of Organic Synthesis , Riga , Latvia.
J Enzyme Inhib Med Chem. 2015 Apr;30(2):216-23. doi: 10.3109/14756366.2014.912214. Epub 2014 Jun 18.
The new histone deacylases inhibitors (HDACi) were synthesized in the class of 5-membered cyclic hydroxamic acids (5-CHA), showing medium size CHA as a new Zn-binding group. New reaction sequence was proposed for the synthesis of 5-membered alkylidene-cyclic-hydroxamic acids starting from butyrolactone. Compound 10c showed low µM activity on HeLa cell extracts. From these results, cyclic hydroxamic acids will be further investigated to find more potent compounds.
新型组蛋白去乙酰化酶抑制剂（HDACi）是在 5 元环羟肟酸（5-CHA）类中合成的，其显示中等大小的 CHA 作为新的 Zn 结合基团。从丁内酯出发，提出了合成 5 元亚烷基-环-羟肟酸的新反应序列。化合物 10c 在 HeLa 细胞提取物中的活性为低 µM。基于这些结果，将进一步研究环状羟肟酸以寻找更有效的化合物。
