[Pt(en)(5-Fu)_2]Cl_2配合物的合成及抗肿瘤活性

Synthesis and Antineoplastic Activity of [Pt(en)(5-Fu)_2]Cl_2

为寻求高效低毒的新型顺铂类抗肿瘤药物,用K2PtCl4、乙二胺(en)、氟尿嘧啶(5-Fu)为原料,设计合成了顺铂类似物[Pt(en)(5-Fu)2]Cl2配合物,由元素分析、红外光谱和质谱分析初步证实了其化学结构,用改良MTT、SRB法,选用K562、A549、Bel-7402、BIU-87、Bcap-37细胞株对其进行体外抗肿瘤活性测定。结果表明,所合成的配合物除在浓度为0.01、0.1μg /mL时对K562细胞株抗肿瘤活性大于顺铂和氟尿嘧啶外,其它情况下的抗肿瘤活性均小于顺铂和氟尿嘧啶。该配合物仍有进一步研究的价值。

In order to find the new antineoplastic medicine with high potential, a low toxic and Pt-based, Pt(Ⅱ)-en-5-Fu complex, as a novel cisplatin complex, was designed and synthesized using K2PtCl4, en, 5-Fu as staring materials. Its antineoplastic activity for the K562, A549, Bel-7402, BIU-87, Bcap-37 cells was measured by the improved MTT, SRB methods. The formula of the complex is [Pt(en)(5-Fu)2]Cl2, the structure has been elucidated by IR spectra , elementary analysis and MS. The antineoplastic activity of Pt(Ⅱ)-en-5-Fu complex is stronger than cisplatin and 5-Fu only in the consistence of 0.01 and 0.1 μg /mL toward K562, and less in other conditions. However , Pt(Ⅱ)-en-5-Fu complex is worthy of being further studied.