A novel dual-functioning ruthenium(II)-arene complex of an anti-microbial ciprofloxacin derivative - Anti-proliferative and anti-microbial activity.
A novel dual-functioning ruthenium(II)-arene complex of an anti-microbial ciprofloxacin derivative - Anti-proliferative and anti-microbial activity.
复制标题
抗微生物环丙沙星衍生物的新型双功能钌 (II)-芳烃复合物 - 抗增殖和抗微生物活性。
DOI：
10.1016/j.jinorgbio.2016.02.018
复制
发表时间：
2016
影响因子：
3.9
通讯作者：
Ude Z
中科院分区：
文献类型：
--
作者：
Ude Z
合成了抗生素环丙沙星的类似物7-（4-（癸酰基）哌嗪-1-基）-环丙沙星（CipA，1）及其钌（Ⅱ）配合物[Ru（η6-p-cymene）（CipA-H）Cl]（2），测定了晶体结构1·1.3H2O·0.6CH3OH和2·CH 3OH·0.5H2O。该配合物具有典型的拟八面体“钢琴凳”构型，Ru（II）π-键合在对伞花烃环上，σ-键合在氟喹诺酮配体的一个氯原子和两个氧原子上。该复合物在低μM范围内具有高度细胞毒性，对人癌细胞系A2780、A549、HCT 116和PC 3的效力与临床药物顺铂相同。它对顺铂和奥沙利铂耐药细胞系也具有高度细胞毒性，表明作用机制不同。该复合物还保留了对人结肠癌细胞系HCT 116 p53的低μM细胞毒性，其中肿瘤抑制因子p53已被敲除，这表明与该复合物相关的有效抗增殖特性与p53的状态无关（与顺铂相反）。该复合物对耐第一、第二和第三代β-内酰胺类抗生素的大肠杆菌、实验室菌株和临床分离株均具有一定的抗菌活性。
7-(4-(Decanoyl)piperazin-1-yl)-ciprofloxacin, CipA, (1) which is an analogue of the antibiotic ciprofloxacin, and its ruthenium(II) complex [Ru(η6-p-cymene)(CipA-H)Cl], (2) have been synthesised and the x-ray crystal structures of1·1.3H2O·0.6CH3OH and2·CH3OH·0.5H2O determined. The complex adopts a typical pseudo-octahedral ‘piano-stool’ geometry, with Ru(II) π-bonded to thep-cymene ring and σ-bonded to a chloride and two oxygen atoms of the chelated fluoroquinolone ligand. The complex is highly cytotoxic in the low μM range and is as potent as the clinical drug cisplatin against the human cancer cell lines A2780, A549, HCT116, and PC3. It is also highly cytotoxic against cisplatin- and oxaliplatin-resistant cell lines suggesting a different mechanism of action. The complex also retained low μM cytotoxicity against the human colon cancer cell line HCT116p53 in which the tumour suppressor p53 had been knocked out, suggesting that the potent anti-proliferative properties associated with this complex are independent of the status of p53 (in contrast to cisplatin). The complex also retained moderate anti-bacterial activity in twoEscherichia coli, a laboratory strain and a clinical isolate resistant to first, second and third generation β-lactam antibiotics.
登录
查看更多内容
影响因子：
16.6
作者：
Debreczeni, JÉ;Bullock, AN;Meggers, E
通讯作者：
Meggers, E
影响因子：
6.9
作者：
Burke, L.;Humphreys, H.;Fitzgerald-Hughes, D.
通讯作者：
Fitzgerald-Hughes, D.
影响因子：
3.5
作者：
Azema, Joelle;Guidetti, Brigitte;Kiss, Robert
通讯作者：
Kiss, Robert
影响因子：
3.2
作者：
Vandecasteele, SJ;Peetermans, WE;Van Eldere, J
通讯作者：
Van Eldere, J
两种新型有机钌(II)配合物的合成、结构表征和细胞毒活性
DOI：
--
发表时间：
2008
期刊：
影响因子：
--
作者：
S. Grgurić;M. Arbi;M. Alshtewi;D. Jeremic;G. Kalud̄erović;S. Gómez‐Ruiz;Ž. Žižak;Z. Juranić;T. Sabo
通讯作者：
T. Sabo