title: 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.affiliation: 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.
authors.forename: Shreelekha
authors.initials: S
authors.lastname: Adsule
authors.forename: Vivek
authors.initials: V
authors.lastname: Barve
authors.forename: Di
authors.initials: D
authors.lastname: Chen
authors.forename: Fakhara
authors.initials: F
authors.lastname: Ahmed
authors.forename: Q Ping
authors.initials: QP
authors.lastname: Dou
authors.forename: Subhash
authors.initials: S
authors.lastname: Padhye
authors.forename: Fazlul H
authors.initials: FH
authors.lastname: Sarkar
mesh_terms: 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
chemical_list: D000447:Aldehydes; D009942:Organometallic Compounds; D061988:Proteasome Inhibitors; D011804:Quinolines; D012545:Schiff Bases; D012663:Semicarbazides; D003300:Copper