钌-乙二胺或邻菲罗啉-氟尿嘧啶配合物的合成及体外抗肿瘤活性

Synthesis of Ru Cl_3-en or Phen-5-Fu in vitro and antineoplastic activity

目的寻求高效低毒的新型钌配合物抗肿瘤药物。方法用RuCl3·3H2O,乙二胺(en)或者邻菲罗啉(Phen),氟尿嘧啶(5-Fu)为原料,设计合成了[Ru(en)(5-Fu)2Cl2]Cl,[Ru(Phen)(5-Fu)2Cl2]Cl配合物。并用改良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。结果合成的[Ru(en)(5-Fu)2Cl2]Cl,[Ru(Phen)(5-Fu)2Cl2]Cl配合物的化学结构由元素分析和红外光谱初步证实。获得配合物细胞株体外抗肿瘤活性数据IC50值。结论[Ru(Phen)(5-Fu)2Cl2]Cl配合物与5-Fu相比,似有进一步研究的价值。

OBJECTIVE: To find the new antineoplastic medicine with high potency, low toxicity and Ru-based. METHODS: [Ru(en) (5-Fu)2Cl2]Cl and [Ru(Phen)(5-Fu)2Cl2]Cl were designed and synthesized, using RuCl3&middot3H2O, en or Phen, 5-Fu as materials. Their antineoplastic activity in vitro for the K562, A549, Bel-7402, BIU-87, Bcap-37 cells was measured with the improved MTT and SRB methods. RESULTS: The compounds were [Ru(en)(5-Fu)2Cl2]Cl and [Ru(Phen)(5-Fu)2Cl2]Cl, and the structures were elucidated by IR spectra and elementary analysis. The IC50 of antineoplastic activity in vitro was obtained. CONCLUSION: Compared with 5-Fu, [Ru(Phen) (5-Fu)2Cl2]Cl complex is worthy of being further studied.