Synthesis and structure confirmation of 7-ester-8-aminomethylene-substituted baicalein derivatives

被引:1
作者
Mou, Jiajia [1 ]
Wang, Qiang [2 ]
Deng, Yanru [1 ]
Chen, Danghui [1 ]
Qiu, Shuang [1 ]
机构
[1] Tianjin Univ Tradit Chinese Med, Sch Chinese Mat Med, Dept Med Chem, Hlth Ind Pk, Tianjin 301617, Peoples R China
[2] South Cent Univ Nationalities, Coll Pharm, Wuhan, Peoples R China
基金
中国国家自然科学基金;
关键词
baicalein derivatives; esterification reaction; Mannich reaction; strontium chloride identification reaction; BIOLOGICAL EVALUATION; CELL-CYCLE; FLAVONOIDS; GROWTH;
D O I
10.1002/jccs.202100194
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Twelve baicalein derivatives, derivatized with 7-ester and 8-aminomethylene groups, were synthesized as cyclin-dependent kinase 1 (CDK1) inhibitors, by the addition of one of four secondary amines to C-8, using the Mannich reaction, followed by mono-esterification with one of three carboxylic acids. Analysis by H-1-, C-13-NMR, and HMBC spectra, as well as a chemical test, confirmed that the esterification occurred at the 7-phenolic hydroxyl position of baicalein but not at the 5- or 6-positions.
引用
收藏
页码:1598 / 1603
页数:6
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