Novel Schiff base copper complexes of quinoline-2 carboxaldehyde as proteasome inhibitors in human prostate cancer cells

被引:366
作者
Adsule, Shreelekha
Barve, Vivek
Chen, Di
Ahmed, Fakhara
Dou, Q. Ping
Padhye, Subhash
Sarkar, Fazlul H.
机构
[1] Wayne State Univ, Sch Med, Barbara Ann Karmanos Canc Inst, Dept Pathol, Detroit, MI 48201 USA
[2] Wayne State Univ, Sch Med, Barbara Ann Karmanos Canc Inst, Prevent Program, Detroit, MI 48201 USA
[3] Univ Pune, Dept Chem, Pune 411007, Maharashtra, India
关键词
D O I
10.1021/jm060712l
中图分类号
R914 [药物化学];
学科分类号
100701 [药物化学];
摘要
We report the synthesis of novel 1: 1 Schiff base copper complexes of quinoline-2-carboxaldehyde showing dose-dependent, antiproliferative, and proapoptotic activity in PC-3 and LNCaP prostate cancer cells. We found that quinoline thiosemicarbazone 2 (FPA-137) was the most potent and inhibited proteosome activity in intact human prostate cancer PC-3 and LNCaP cells (IC50 of 4 and 3.2 mu M, respectively) compared to clioquinol and pyrrolidine dithiocarbamate (IC50 of 10 and 20 mu M), supporting the novelty of 2.
引用
收藏
页码:7242 / 7246
页数:5
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