以磺酰胺和酰胺键为连接单元、靶向组蛋白去乙酰化酶的肉桂酰羟肟酸衍生物的合成

Nguyen Cuong Quoc, Le Dang Quang, Nguyen Duy Tuan, Trần Duy Khang, Nguyen Vu Linh, Tran Thanh Men, Nguyen Trong Tuan, B. Hue, Tran Quang De
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引用次数: 0

摘要

基于贝利诺司他的强大活性,研究人员合成了一些肉桂酰羟肟酸衍生物,目的是创造出具有选择性抑制 HDAC 的潜力的新化合物,为癌症治疗做出贡献。 N-羟基肉桂酰胺既是ZBG,又是连接基团。这些衍生物通过分子对接与 HDAC2 和 HDAC8 酶定向。化合物 9a(含磺酰胺)是最有可能抑制 HDAC2 酶功能的候选化合物。
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Synthesis of Cinnamoylhydroxamic Acid Derivatives Bearing Sulfonamide, Amide Bonds as Connecting Unit Targeting Histone Deacetylases
Based on the strong activity of belinostat, the study synthesized of some cinnamoylhydroxamic acid derivatives with the aim of creating new compounds that have the potential to selectively inhibit HDAC to contribute to cancer treatment.  N-hydroxycinnamamide serves as both ZBG and the linker group. The derivatives orient to the HDAC2 and HDAC8 enzymes by molecular docking. Compound 9a (bearing sulfonamide) exhibited as the most potential candidate to inhibit the function of HDAC2 enzyme.
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