Department of Chemistry, University of Fribourg, Chemin du Musée 10, 1700 Fribourg, Switzerland.
Department of experimental oncology, Institute for Oncology and Radiology of Serbia, Pasterova 14, Beograd, Republic of Serbia.
Dalton Trans. 2023 May 22;52(20):6934-6944. doi: 10.1039/d2dt04041g.
We report the synthesis, characterization, and evaluation of the anticancer activity of a series of 5- and 6-(halomethyl)-2,2'-bipyridine rhenium tricarbonyl complexes. The study was promoted in order to understand if the presence and position of a reactive halomethyl substituent on the diimine ligand system of -[Re(CO)] species may be a key molecular feature for the design of active and non-toxic anticancer agents. Only compounds potentially able to undergo ligand-based alkylating reactions show significant antiproliferative activity against colorectal and pancreatic cell lines. Of the new species presented in this study, one compound (5-(chloromethyl)-2,2'-bipyridine derivative) shows significant inhibition of pancreatic tumour growth in zebrafish-Panc-1 xenografts. The complex is noticeably effective at 8 μM concentration, lower than its IC values, being also capable of inhibiting cancer cells dissemination.
我们报告了一系列 5-和 6-（卤代甲基）-2,2'-联吡啶铼三羰基配合物的合成、表征和抗癌活性评价。这项研究的目的是了解二亚胺配体系统上的卤代甲基取代基的存在和位置是否可能是设计活性和无毒抗癌药物的关键分子特征。只有那些可能发生配体基烷基化反应的化合物对结直肠和胰腺细胞系表现出显著的增殖抑制活性。在本研究中提出的新化合物中，一种化合物（5-（氯甲基）-2,2'-联吡啶衍生物）在斑马鱼-Panc-1 异种移植中显示出对胰腺肿瘤生长的显著抑制作用。该配合物在 8 μM 的浓度下具有显著的效果，低于其 IC 值，并且还能够抑制癌细胞的扩散。
