当前位置: X-MOL 学术J. Inorg. Biochem. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
First dinuclear rhodium(II) complexes with triazolopyrimidines and the prospect of their potential biological use.
Journal of Inorganic Biochemistry ( IF 3.8 ) Pub Date : 2020-03-23 , DOI: 10.1016/j.jinorgbio.2020.111072
Marzena Fandzloch 1 , Adam W Augustyniak 2 , Liliana Dobrzańska 3 , Tomasz Jędrzejewski 4 , Jerzy Sitkowski 5 , Magdalena Wypij 6 , Patrycja Golińska 6
Affiliation  

Five novel rhodium(II) complexes of general formula [Rh2(μ-OOCCH3)4L2], where L is a triazolopyrimidine derivative, in particular dimethyl-1,2,4-triazolo[1,5-a]pyrimidine (dmtp) for (1), 5,7-diethyl-1,2,4-triazolo[1,5-a]pyrimidine (detp) for (2), 7-isobutyl-5-methyl-1,2,4-triazolo[1,5-a]pyrimidine (ibmtp) for (3), 7-hydroxy-5-methyl-1,2,4-triazolo[1,5-a]pyrimidine (HmtpO) for (4) and 5,7-ditertbutyl-1,2,4-triazolo[1,5-a]pyrimidine (dbtp) for (5) are reported. These first representatives of paddle-wheel dirhodium complexes with triazolopyrimidines have been characterized by IR and NMR spectroscopy as well as by single-crystal X-ray diffraction studies. Three of the new complexes (1), (2) and (5) were thoroughly screened in vitro for their cytotoxicity against human breast cancer cell line MCF-7 and L929 murine fibroblast cells. Favorably, they show significantly less effective inhibition on the cell growth of L929 than cisplatin under identical conditions. Complexes (1) and (5) display moderate cytotoxic activity (IC50 = 16.3–21.5 μM) against MCF-7 cells which is induced via reactive oxygen species-independent pathways. Extensive studies of rhodium complexes (1), (2) and (5) against microorganisms have shown that the tested compounds exhibit antibacterial activity against Gram-positive bacteria (Staphylococcus aureus and Bacillus subtilis) while (5) significantly inhibited the growth of Malassezia furfur. The highest antibacterial, and antifungal activity, was observed for (5).



中文翻译:

第一种双核铑(II)与三唑并嘧啶的络合物及其潜在生物用途的前景。

五个新颖铑(II)通式的配合物的[Rh 2(μ-OOCCH 34大号2 ],其中L为三唑并嘧啶衍生物,特别是二甲基-1,2,4-三唑并[1,5]嘧啶(dmtp)对于(1),5,7-二乙基-1,2,4-三唑[1,5- a ]嘧啶(detp)对于(2),7-异丁基-5-甲基-1,2,4 -三唑并[1,5-一个]嘧啶(ibmtp)对于(3),7-羟基-5-甲基-1,2,4-三唑并[1,5]嘧啶(HmtpO)为(4)和5 ,7-二叔丁基-1,2,4-三唑并[1,5-一个]嘧啶(dbtp)为(5)报告。这些具有三唑并嘧啶的叶轮吡啶鎓络合物的第一批代表物已通过IR和NMR光谱以及单晶X射线衍射研究进行了表征。在体外彻底筛选三种新复合物(1),(2)和(5)对人乳腺癌细胞系MCF-7和L929鼠成纤维细胞的细胞毒性。有利地,在相同条件下,它们对L929细胞生长的抑制作用明显小于顺铂。配合物(1)和(5)显示中等的细胞毒活性(IC 50 = 16.3–21.5μM)针对MCF-7细胞,这是通过与活性氧无关的途径诱导的。铑配合物(1),(2)和(5)对微生物的广泛研究表明,所测试的化合物对革兰氏阳性细菌(金黄色葡萄球菌枯草芽孢杆菌)具有抗菌活性,而(5)显着抑制糠Mal马拉色菌的生长。观察到最高的抗菌和抗真菌活性(5)。

更新日期:2020-03-23
down
wechat
bug