新型手性配体衍生的抗肿瘤双核铂(II)配合物。
Antitumor dinuclear platinum(II) complexes derived from a novel chiral ligand.
机构信息
Pharmaceutical Research Center and School of Chemistry and Chemical Engineering, Southeast University, Nanjing 211189, China.
出版信息
Bioorg Med Chem Lett. 2011 Nov 1;21(21):6386-8. doi: 10.1016/j.bmcl.2011.08.100. Epub 2011 Aug 28.
A new chiral ligand, 2-(((1R,2R)-2-aminocyclohexyl)amino)acetic acid (HL), was designed and synthesized to prepare a series of novel dinuclear platinum(II) complexes with dicarboxylates or sulfate as bridges. The evaluation of these metal complexes in vitro cytotoxicity against human HCT-116, MCF-7 and HepG-2 cell lines were made. All compounds showed antitumor activity to HCT-116 and MCF-7. Particularly, compounds M3 and M5 not only exhibited better activity than carboplatin against MCF-7 and HepG-2, but also showed very close activity to oxaliplatin against HCT-116.
一种新的手性配体，2-(((1R,2R)-2-氨基环己基)氨基)乙酸（HL），被设计和合成，以制备一系列具有二羧酸或硫酸盐桥的新型双核铂（II）配合物。对这些金属配合物在体外对人 HCT-116、MCF-7 和 HepG-2 细胞系的细胞毒性进行了评价。所有化合物对 HCT-116 和 MCF-7 均显示出抗肿瘤活性。特别是化合物 M3 和 M5 不仅对 MCF-7 和 HepG-2 的活性优于顺铂，而且对 HCT-116 的活性与奥沙利铂非常接近。
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