Novel Schiff base copper complexes of quinoline-2 carboxaldehyde as proteasome inhibitors in human prostate cancer cells.
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.
Adsule
Shreelekha
S
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.
Barve
Vivek
V
Chen
Di
D
Ahmed
Fakhara
F
Dou
Q Ping
QP
Padhye
Subhash
S
Sarkar
Fazlul H
FH
D000447:Aldehydes / Q000737:chemistry*; D045744:Cell Line, Tumor; D003300:Copper; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D008297:Male; D009942:Organometallic Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011471:Prostatic Neoplasms; D061988:Proteasome Inhibitors; D011804:Quinolines / Q000737:chemistry*; D012545:Schiff Bases / Q000737:chemistry*; D012663:Semicarbazides / Q000737:chemistry; D013329:Structure-Activity Relationship
D000447:Aldehydes; D009942:Organometallic Compounds; D061988:Proteasome Inhibitors; D011804:Quinolines; D012545:Schiff Bases; D012663:Semicarbazides; D003300:Copper