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

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

  • J Med Chem. 2006 Nov 30;49(24):7242-6. doi: 10.1021/jm060712l.
Shreelekha Adsule 1,  Vivek Barve,  Di Chen,  Fakhara Ahmed,  Q Ping Dou,  Subhash Padhye,  Fazlul H Sarkar
Affiliations

Affiliation

  • 1 The Prevention Program and Department of Pathology, Barbara Ann Karmanos Cancer Institute, Wayne State University, School of Medicine, 9374 Scott Hall, 540 East Canfield Avenue, Detroit, Michigan 48201, USA.
PMID: 17125278 DOI: 10.1021/jm060712l
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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