新型铂(Ⅱ)类配合物的合成、表征和抗肿瘤活性

Synthesis,Characterization and Antitumor Activities of New Type Platinum(II) Complexes

0引言 1967年发现顺铂,即铂族金属配合物顺式-二氯二氨合铂(Ⅱ),具有抗肿瘤活性后,于1971年进入Ⅰ期临床试验,7年后获准用于治疗睾丸肿瘤和卵巢癌.

Seven novel platinum（Ⅱ） complexes[Pt（Ⅱ）（NH3）（H2O）X]（Ⅰ-Ⅶ） {X=（COO^-）2（oxalato）, 2p-CH3O-C6H4-COO^- （p-methyoxbenzolato）, 2C6H5-COO^-（benzolato）, 2CH3COO^-（acetato）, （CH2） （COO^-）2 （malonato）, （CH2）2 （COO^-）2 （succinato）, （CH=CH）（COO^-）2（maleato）} have been prepared and characterized by elemental analysis, thermal analysis,IR, UV, and ^1H NMR spectroscopy. The antitumor activities of these complexes in vitro against EJ.HCT-8, KB, BGC-823, Bel-7402, HL-60, MCF-7 and Hela cell lines have been studied. Complex Ⅰ and Ⅴ show remarkable antitumor activities against EJ cell line, and the inhibitory rate is 45.96% and 54.32% at concentration of 10μmol·L^-1, respectively. The inhibitory, rate of the complexes Ⅱ and Ⅲ is greater than 50% against HL-60, BGC-823, KB and EJ cell lines. The inhibitory rate of the complex Ⅳ is 51.89% and 57.96% against BGC-823 and EJ cell lines. The complexes Ⅳ and Ⅶ have no antitumor activities against tested tumor cell lines. The complexes Ⅱ, Ⅲ and Ⅳ can stem the cell cycle of HL-60 on the G2＋M.