Synthesis and preliminary studies of biological activity of amino derivatives of 4-azatricyclo- [5.2.1.02,6]dec-8-ene-3,5-dione with silicon in the structure

Heterocyclic communications

article

Mariola Napiórkowska¹  Marcin Cieślak²  Julia Kaźmierczak-Barańska²  Karolina Królewska²  Aleksandra Czapla³  Bożena Kuran³ 

[1] Department of Biochemistry, Medical University of Warsaw;Department of Bioorganic Chemistry, Centre of Molecular and Macromolecular Studies, Polish Academy of Sciences;Department of Medical Chemistry, Medical University of Warsaw

关键词: cytotoxic activity;    HeLa;    5-HT1A ligands;    5-HT7 ligands;    K562;    organosilicon compounds;   

DOI  :  10.1515/hc-2014-0144

学科分类：内科医学

来源: De Gruyter

【 摘 要 】

A series of 38 new derivatives of cyclic imides containing silicon in the structure was synthesized and characterized by 1 H NMR, ESI-MS, and elemental analysis. Selected compounds ( 1l,m , 1g , 1o,p , 2l,m , and 2o,p ) were tested for their cytotoxic properties in human chronic myelogenous leukemia (K562), human cervical cancer (HeLa), and normal endothelial cells (HUVEC). Seven compounds showed significant cytotoxicity. In addition, two compounds ( 1l and 2l ) were tested toward affinity for 5-HT 1A , 5-HT 6 , and 5-HT 7 serotonin receptors, and all aryl/heteroarylopiperazino derivatives were tested for antimicrobial activity. The compounds tested toward affinity for selected serotonin receptors showed high and moderate affinity for 5-HT 1A and 5-HT 7 , while the antimicrobial activity of tested compounds was not significant.

【 授权许可】

CC BY|CC BY-NC-ND