25307-03-3Relevant articles and documents
Dual investigation of lanthanide complexes with cinnamate and phenylacetate ligands: Study of the cytotoxic properties and the catalytic oxidation of styrene
Aragón-Muriel, Alberto,Camprubí-Robles, María,González-Rey, Elena,Salinas-Castillo, Alfonso,Rodríguez-Diéguez, Antonio,Gómez-Ruiz, Santiago,Polo-Cerón, Dorian
, p. 117 - 128 (2014)
Eleven lanthanide compounds [Y(cinn)3] (1), [La(cinn) 3] (2), [La(4-OMecinn)3]·2H2O (3), [La(4-Clcinn)3]·2H2O (4), [La(4-OMephac) 3]·4H2O (5), [La(4-Clphac)3] ·3H2O (6), [Ce(cinn)3] (7), [Nd(cinn)3] (8), [Sm(cinn)3]·H2O (9), [Yb(cinn)3] (10) and [Sm(4-OMephac)3]·H2O (11) containing carboxylato ligands (cinn = cinnamate; 4-OMecinn = 4-methoxicinnamate; Clcinn = 4-chlorocinnamate; 4-OMephac = 4-methoxyphenylacetate; 4-Clphac = 4-chlorophenylacetate) have been synthesized and characterized by elemental analysis, IR, 1H and 13C NMR spectroscopy, thermal analysis and X-ray diffraction powder patterns. In addition, compound 11 was characterized by single crystal X-ray diffraction studies. The cytotoxic activity of these complexes has been tested against three different human tumour cell lines HL60 (human promyelocytic leukemia), K562 (human erythromyeloblastoid leukemia) and MCF7 (breast cancer), observing a very modest cytotoxic activity for all tested compounds. In addition, toxicity tests to macrophages and erythrocytes have also been carried out, observing that none of the compounds is toxic against these immunocompetent cells. Finally, all the synthesized compounds have been tested as catalysts for styrene oxidation observing conversions higher than 50% after 19 h of reaction as well as a relatively high selectivity to two main products benzaldehyde (BzA) and 1-phenylethane-1,2-diol (PhED). Complex 7 presents the higher conversion (99.56%) with a relatively high selectivity towards PhED of 72.07%.
Novel 3-arylfuran-2(5H)-one-fluoroquinolone hybrid: Design, synthesis and evaluation as antibacterial agent
Wang, Xu-Dong,Wei, Wei,Wang, Peng-Fei,Tang, Yun-Tao,Deng, Rui-Cheng,Li, Biao,Zhou, Sha-Sha,Zhang, Jing-Wen,Zhang, Lei,Xiao, Zhu-Ping,Ouyang, Hui,Zhu, Hai-Liang
, p. 3620 - 3628 (2014/07/07)
3-Arylfuran-2(5H)-one, a novel antibacterial pharmacophore targeting tyrosyl-tRNA synthetase (TyrRS), was hybridized with the clinically used fluoroquinolones to give a series of novel multi-target antimicrobial agents. Thus, twenty seven 3-arylfuran-2(5H)-one-fluoroquinolone hybrids were synthesized and evaluated for their antimicrobial activities. Some of the hybrids exhibited merits from both parents, displaying a broad spectrum of activity against resistant strains including both Gram-negative and Gram-positive bacteria. The most potent compound (11) in antibacterial assay shows MIC50 of 0.11 μg/mL against Multiple drug resistant Escherichia coli, being about 51-fold more potent than ciprofloxacin. The enzyme assays reveal that 11 is a potent multi-target inhibitor with IC50 of 1.15 ± 0.07 μM against DNA gyrase and 0.12 ± 0.04 μM against TyrRS, respectively. Its excellent inhibitory activities against isolated enzymes and intact cells strongly suggest that 11 deserves to further research as a novel antibiotic.