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

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• 作者：Bojana B. Krajč ; inović ; Goran N. Kaluđ ; erović ; Dirk Steinborn ; Harry Schmidt ; Christoph Wagner ; Ž ; eljko Ž ; iž ; ak ; Zorica D. Juranić ; Sreć ; ko R. Trifunovi
• 关键词：Platinum(II) complexes ; Platinum(IV) complexes ; Antitumoral activity ; Edda ligands
• 刊名：Journal of Inorganic Biochemistry
• 出版年：2008
• 期刊代码：53_01620134
• 类别：ch
• 出版时间：April 2008
• 卷：102
• 期：4
• 页码：892-900
• 文件大小：562 K

摘要

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, ¹H and ¹³C 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 IC₅₀(μM) 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.