具有动态生物活性谱的基于硫醇盐的α-羟基托酚酮文库的发散合成。
Divergent synthesis of a thiolate-based α-hydroxytropolone library with a dynamic bioactivity profile.
作者信息
Agyemang Nana B, Kukla Cassandra R, Edwards Tiffany C, Li Qilan, Langen Madison K, Schaal Alexandra, Franson Abaigeal D, Casals Andreu Gazquez, Donald Katherine A, Yu Alice J, Donlin Maureen J, Morrison Lynda A, Tavis John E, Murelli Ryan P
机构信息
Department of Chemistry, Brooklyn College, The City University of New York, Brooklyn, New York 11210, United States.
PhD Program in Chemistry, The Graduate Center of The City University of New York, New York, New York 10016, United States.
出版信息
RSC Adv. 2019;9(59):34227-34234. doi: 10.1039/c9ra06383h. Epub 2019 Oct 23.
Here we describe a rapid and divergent synthetic route toward structurally novel αHTs functionalized with either one or two thioether or sulfonyl appendages. Evaluation of this library against hepatitis B and herpes simplex virus, as well as the pathogenic fungus , and a human hepatoblastoma (HepDES19) revealed complementary biological profiles and new lead compounds with sub-micromolar activity against each pathogen.
在此，我们描述了一种快速且多样化的合成路线，用于合成结构新颖的αHTs，其带有一个或两个硫醚或磺酰基附属物进行功能化修饰。对该化合物库针对乙型肝炎病毒、单纯疱疹病毒以及致病真菌和人肝母细胞瘤（HepDES19）进行评估，结果显示出互补的生物学特性以及对每种病原体具有亚微摩尔活性的新型先导化合物。
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