期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 30, 期 4, 页码 -出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2019.126925
关键词
Topoisomerase 1; Indole-pyrazoline hybrid derivatives; CPT; Supercoiled DNA
资金
- Guangdong Medical Research Fund [B2019003]
- Guangdong Provincial Education Department Fund [51340208]
A series of novel indole-pyrazoline hybrid derivatives were designed, synthesized, and evaluated for topoisomerase 1 (Top1) inhibitory activity. Top1-mediated relaxation assays showed that our synthesized compounds had variable Top1 inhibitory activity. Among these compounds, 3-(5-(naphthalen-1-yl)-1-phenyl-4,5-dihydro-1H-pyrazol-3-yl)-1-(phenylsulfonyl)-1H-indole (6n) was found to be a strong Top1 inhibitor with better inhibitory activity than CPT and hit compounds. Our further experiments rationalized the mode of action for this new type of inhibitors, which showed no significant binding to supercoiled DNA.
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