1349703-45-2Relevant articles and documents
Application of N-heterocyclic carbene selenium-gold compound in preparation of carbapenem-resistant acinetobacter baumannii drug
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Paragraph 0024; 0029-0031; 0036; 0038, (2021/07/21)
The invention discloses application of an N-heterocyclic carbene selenium-gold compound in preparation of a novel antibacterial drug resistant to carbapenem acinetobacter baumannii infection, and belongs to the technical field of drug preparation. According to the N-heterocyclic carbene selenium-gold compound, selenium-containing imidazole N-heterocyclic carbene selenium is used for replacing a thiosaccharide ligand in a gold nofen structure; the reaction activity of Au-Se in the N-heterocyclic carbene selenium-gold compound is higher than that of an Au-S bond, so that the Au-S bond in a Jinnofen structure can be prevented from being easily damaged by reducing mercaptan to a certain extent; and toxic and side effects are caused by metabolism before reaching a target spot. In-vitro antibacterial activity shows that IC50 of the compounds H7 and H8 in inhibition of carbapenem-resistant acinetobacter baumannii is 3.34 mu M and 4.67 mu M, MIC of the same are both 10 mu M, and MBC of the same are both 20 mu M. The animal in-vivo administration also shows a good anti-drug-resistant bacterium effect, which proves that the compound can significantly prolong the survival time of mice infected by drug-resistant bacteria, and has important practical application value.
A new rhodium(I) NHC complex inhibits TrxR: In vitro cytotoxicity and in vivo hepatocellular carcinoma suppression
Fan, Rong,Bian, Mianli,Hu, Lihong,Liu, Wukun
, (2019/10/01)
Thioredoxin reductase (TrxR) is often overexpressed in different types of cancer cells including hepatocellular carcinoma (HCC) cells and regarded as a target with great promise for anticancer drug research and development. Here, we have synthesized and characterized nine new designed rhodium(I) N-heterocyclic carbene (NHC) complexes. All of them were effective towards cancer cells, especially complex 1e was more active than cisplatin and manifested strong antiproliferative activity against HCC cells. In vivo anticancer studies showed that 1e significantly repressed tumor growth in an HCC nude mouse model and ameliorated liver lesions in a chronic HCC model caused by CCl4. Notably, a mechanistic study revealed that 1e can strongly inhibit TrxR system both in vitro and in vivo. Furthermore, 1e promoted intracellular ROS accumulation, damaged mitochondrial membrane potential, promoted cancer cell apoptosis and blocked the cells in the G1 phase.
Synthesis and biological studies of silver N-heterocyclic carbene complexes derived from 4,5-diarylimidazole
Liu, Wukun,Bensdorf, Kerstin,Hagenbach, Adelheid,Abram, Ulrich,Niu, Ben,Mariappan, Aruljothi,Gust, Ronald
, p. 5927 - 5934 (2012/01/02)
A novel class of silver N-heterocyclic carbene complexes (5a-f) were synthesized in high yield by reacting silver(I) oxide with 4,5-diarylimidazolium halides (4a-f). The complexes were characterized using NMR and IR spectroscopy. The structure was confirmed on the example of bromo[1,3-diethyl-4,5-bis(4- fluorophenyl)imidazol-2-ylidene]silver(I) (5c) by crystal structure analysis. The X-ray structure indicated a three-dimensional coordination polymer with a repeating unit consisting of a Ccarben-Ag2-Br 2-Ccarben cluster. Pharmacological investigations revealed that all silver complexes possessed growth inhibitory effects against breast cancer (MCF-7 and MDA-MB-231) as well as colon carcinoma (HT-29) cells. The most active compound 5c was slightly less active against MCF-7 cells, more active against MDA-MB-231 cells and comparable active as cisplatin against HT-29 cells. Further pharmacological investigations were performed with selected compounds on estrogen receptor (ER) binding, DNA intercalation, cyclooxygenase (COX) inhibition and antibacterial activity. The complexes were only marginally active at the DNA, ER and the COX enzymes, so these targets can be excluded to be involved in the mode of action. However, the growth of bacteria was significantly inhibited by 5c and 5f and opens a new application of this complex type.
