Development of anticancer platinum complexes that recognize a specific region of nucleic acid.

我们合成了一系列四氮杂双核铂(II)配合物作为一类新的化合物，以开发新一代基于铂的抗癌药物，这些药物对通常对化疗耐药的癌症有效。以H460非小细胞肺癌和PANC-1胰腺癌移植瘤为模型，评价了其中一种化合物的体内抗肿瘤作用。该化合物对胰腺癌具有明显的抗肿瘤作用。四氮唑桥联化合物与DNA的相互作用方式与临床铂类药物不同。

We have synthesized a series of tetrazolate-bridged dinuclear Pt(II) complexes as a new class, in order to develop next-generation platinum-based anticancer drugs which are effective against cancers that are typically resistant to chemotherapy. In vivo antitumor efficacy of one of the complexes was evaluated on xenografted tumors of H460 non-small cell lung cancer and PANC-1 pancreatic cancer. The complex exhibited markedly high antitumor efficacy against pancreatic cancer. The tetrazolate-bridged complexes resulted to interact with DNA in a manner different from that of clinical platinum-based drugs.