Synthesis and in vitro antitumoral activity of novel O,O'-di-2-alkyl-(S,S)-ethylenediamine-N,N'-di-2-propanoate ligands and corresponding platinum(II/IV) complexes.
Syntheses of two novel ligand precursors O,O'-diisopropyl- (1a) and O,O'-diisobutyl-(S,S)-ethylenediamine-N,N'-di-2-propanoate dihydrochloride monohydrate (1b) and the corresponding dichloroplatinum(II) (2a and 2b) and tetrachloroplatinum(IV) complexes (3a and 3b) are described here. The substances were characterized by IR, (1)H and (13)C spectroscopy and elemental analysis. Crystal structures were determined for 1a and the corresponding platinum(IV) complex, 3a. In vitro antiproliferative activity was determined against tumor cell lines: human adenocarcinoma HeLa, human myelogenous leukemia K562, human malignant melanoma Fem-x, rested and stimulated normal immunocompetent cells (human peripheral blood mononuclear PBMC cells) using KBR test (Kenacid Blue Dye binding test). The IC(50)(microM) values for the most active compound 3a were: 30.48+/-2.54; 12.26+/-2.60; 13.68+/-3.22; 80.18+/-24.07 and 71.30+/-21.70, respectively.
Krajcinović
Bojana B
BB
Department of Chemistry, Institute of Chemistry, Technology and Metallurgy, Studentski trg 14, 11000 Belgrade, Serbia.
Kaluderović
Goran N
GN
Steinborn
Dirk
D
Schmidt
Harry
H
Wagner
Christoph
C
Zizak
Zeljko
Z
Juranić
Zorica D
ZD
Trifunović
Srećko R
SR
Sabo
Tibor J
TJ
D018360:Crystallography, X-Ray; D006367:HeLa Cells; D006801:Humans; D008024:Ligands; D009682:Magnetic Resonance Spectroscopy; D008958:Models, Molecular; D015394:Molecular Structure; D009944:Organoplatinum Compounds / Q000138:chemical synthesis* / Q000494:pharmacology*; D011422:Propionates / Q000138:chemical synthesis* / Q000494:pharmacology*; D013055:Spectrophotometry, Infrared
D008024:Ligands; D009944:Organoplatinum Compounds; D011422:Propionates