A range of precious metal complexes incorporating either benzyl or carbaboranyl functionalised tethered N-heterocyclic carbenes have been prepared, including single X-ray crystallography for one new complex. The library has been screened for their anti-cancer potential against colorectal, ovarian, cisplatin-resistant ovarian and breast cancer cell lines and their selectivity determined by comparing the cytotoxicity towards normal cells. Overall, these complexes show significant selectivity for ovarian carcinoma, and are up to 3-fold more cytotoxic than cisplatin against cisplatin-resistant human ovarian carcinoma. Upon replacing the benzyl moiety of the NHC ligand with a carbaboranyl there is a general increase observed in the potency of the complexes, with the cytotoxicity of the ruthenium complex increasing by > 16-fold against human ovarian carcinoma. Generally, the rhodium complex with the benzyl tethered NHC shows the greatest selectivity for cancer, with a selectivity index of 15, which is > 2x, >9x and >6x higher than that of cisplatin, carboplatin and oxaliplatin, respectively.

已经制备了一系列结合了苄基或碳酰氨基官能化的N-杂环卡宾的贵金属配合物，包括一个新配合物的单X射线晶体学。已筛选该文库对结肠直肠癌，卵巢癌，顺铂耐药性卵巢癌和乳腺癌细胞系的抗癌潜力，并通过比较对正常细胞的细胞毒性来确定其选择性。总体而言，这些复合物对卵巢癌显示出显着的选择性，并且对顺铂耐药的人卵巢癌的细胞毒性比顺铂高三倍。将NHC配体的苄基部分替换为碳酰氨基后，发现复合物的效力普遍增加，而钌复合物的细胞毒性则增加> 抗人卵巢癌的能力是其的16倍。通常，具有苄基拴系NHC的铑配合物显示出对癌症的最大选择性，其选择性指数为15，分别比顺铂，卡铂和奥沙利铂高2倍，9倍和6倍以上。