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. 2006 Nov 30;49(24):7242-6.
doi: 10.1021/jm060712l.

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

Shreelekha Adsule  1 , Vivek Barve, Di Chen, Fakhara Ahmed, Q Ping Dou, Subhash Padhye, Fazlul H Sarkar
Affiliations

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

Shreelekha Adsule et al. J Med Chem. .

Abstract

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 microM, respectively) compared to clioquinol and pyrrolidine dithiocarbamate (IC50 of 10 and 20 microM), supporting the novelty of 2.

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