In vitro cytotoxicity study on platinum (II) complexes with epoxysuccinates as leaving groups.
A series of novel cisplatin-type platinum complexes were designed, characteristic of epoxysuccinates as leaving groups. The pertinent compounds were prepared and characterized by IR, (1)H NMR, and ESI-MS spectra with elementary analyses. The in vitro cytotoxic activities of compounds toward SPC-A1 human lung adenocarcinoma cell line and BGC823 human stomach adenocarcinoma cell line were determined. Biological tests have confirmed that complexes containing 4R,5R-DMID [abbreviation of (4R,5R)-4,5-bis (aminomethyl)-2-isopropyl-1,3-dioxolane] as carrier ligands have greater cytotoxicity toward tumor cells than the corresponding compounds with other carrier ligands. Most platinum complexes with trans-epoxysuccinates usually have higher cytotoxicity than those with cis-epoxysuccinates. Complex 4a shows the most effective among those tested platinum complexes in both cell lines, and its cytotoxicity approached that of cisplatin.
Liu
Xia
X
State Key Laboratory of Coordination Chemistry, Nanjing University, Nanjing 210093, China.
Shen
Hong
H
Zhu
Haibin
H
Cui
Kai
K
Gou
Shaohua
S
D000230:Adenocarcinoma / Q000473:pathology; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D004852:Epoxy Compounds / Q000737:chemistry*; D006801:Humans; D066298:In Vitro Techniques; D008175:Lung Neoplasms / Q000473:pathology; D009682:Magnetic Resonance Spectroscopy; D017671:Platinum Compounds / Q000737:chemistry / Q000494:pharmacology*; D021241:Spectrometry, Mass, Electrospray Ionization; D013386:Succinates / Q000737:chemistry*
D000970:Antineoplastic Agents; D004852:Epoxy Compounds; D017671:Platinum Compounds; D013386:Succinates