Shanghai Key Laboratory of Green Chemistry and Chemical Process, School of Chemistry and Molecular Engineering , East China Normal University , 3663 North Zhongshan Road , Shanghai 200062 , P.R. China.
Department of Chemical Engineering and Biotechnology , University of Applied Sciences Darmstadt , Darmstadt 64295 , Germany.
Org Lett. 2019 Sep 20;21(18):7484-7488. doi: 10.1021/acs.orglett.9b02784. Epub 2019 Sep 9.
An efficient and practical thiocarbonyl surrogate via combination of potassium sulfide and chloroform was established. A variety of dithiocarbamates were afforded along with four new chemical bond formations in a one-pot reaction in which the thiocarbonyl motif was generated in situ. Furthermore, these readily accessed molecules showed promising activity against HDAC8, opening a potential gateway to discover a new type of nonhydroxamate and isoenzyme-selective HDAC inhibitors.
建立了一种高效实用的通过硫化钾和氯仿组合的硫羰基替代物。在一锅反应中，原位生成硫羰基，同时形成了四个新的化学键，生成了各种二硫代氨基甲酸盐。此外，这些易于获得的分子对 HDAC8 表现出了有前景的活性，为发现新型非羟肟酸和同工酶选择性 HDAC 抑制剂开辟了潜在途径。
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