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

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.

• Authors: Shreelekha Adsule, Vivek Barve, Di Chen, Fakhara Ahmed, Q Ping Dou, Subhash Padhye, Fazlul H Sarkar
• Journal: Journal of medicinal chemistry (J Med Chem) Vol. 49 Issue 24 Pg. 7242-6 (Nov 30 2006) ISSN: 0022-2623 [Print] United States
• PMID: 17125278 (Publication Type: Journal Article)

Chemical References

• Aldehydes
• Organometallic Compounds
• Proteasome Inhibitors
• Quinolines
• Schiff Bases
• Semicarbazides
• Copper

Topics

• Aldehydes (chemistry)
• Cell Line, Tumor
• Copper
• Drug Screening Assays, Antitumor
• Humans
• Male
• Organometallic Compounds (chemical synthesis, chemistry, pharmacology)
• Prostatic Neoplasms
• Proteasome Inhibitors
• Quinolines (chemistry)
• Schiff Bases (chemistry)
• Semicarbazides (chemistry)
• Structure-Activity Relationship