The Experts below are selected from a list of 27 Experts worldwide ranked by ideXlab platform
Juan Server-carrió - One of the best experts on this subject based on the ideXlab platform.
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Potentiometric and spectroscopic studies of transition-metal ions complexes with a Quinolone Derivative (cinoxacin). Crystal structures of new Cu(II) and Ni(II) cinoxacin complexes
Journal of Inorganic Biochemistry, 1997Co-Authors: M. Ruiz, R. Ortiz, L. Perelló, Julio Latorre, Juan Server-carrióAbstract:Abstract The interaction of cobalt(II), nickel(II), copper(II), and zinc(II) with Cinoxacin (HCx = 1-ethyl-1,4-dihydro-4-oxo(1,3)dioxolo(4,5-g)cinnoline-3-carboxylic acid), a 4-Quinolone Derivative, has been studied at metal/ligand ratios of 1:1-1:3 by means of pH-metric, spectrophotometric, and ESR methods. The formation constants have been determined and the stereochemistry for the metal ions in the species present in aqueous solutions (at 37 ± 0.1°C and I = 0.1 mol dm −3 NaCl) is discussed. In all the studied systems, complexes with different stoichiometric ratios, in which cinoxacin acts both as neutral and deprotonated ligand, are formed. The anomalous sequence of the stepwise stability constants observed for cobalt(II) and nickel(II) systems suggests changes in stereochemistry when CoCx 2 and NiCx 2 are formed. For zinc(II) this change has to be still more pronounced since a [ZnCx] + species has not been detected. For the Cu(II) system the sequence in the stepwise stability constants indicates the preferential formation of the [CuCx] + monocomplex. The crystal and molecular structure of new Cu(II) and Ni(II) complexes of cinoxacin have been investigated. The metal ion in [Cu(Cx) 2 H 2 O]·3H 2 O is five-coordinated and the complex crystallizes in the triclinic P 1 space group with a = 10.620(1), b = 11.358(1), c = 12.440(2) A , α = 78.25(1), β = 80.24(1), γ = 63.34(1)°, and Z = 2 . The complex [Ni(Cx) 2 -(DMSO) 2 ]·4H 2 O contains six-coordinated Ni(II) and crystallizes in the triclinic P 1 space group with a = 8.866(3), b = 9.141(1), c = 11.580(1) A , α = 69.301(9), β = 82.17(2), γ = 75.86(2)°, and Z = 1 .
Jacek Musiał - One of the best experts on this subject based on the ideXlab platform.
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Treatment of respiratory tract infections with pefloxacin
Polskie Archiwum Medycyny Wewnetrznej, 1991Co-Authors: W Królikowski, Piotr Głuszko, Jerzy Soja, A Prokop, M Wandzilak, T Klisiewicz-pańszczyk, I Jurek, M Gruszka, S Sek, Jacek MusiałAbstract:Pefloxacin, a 4-Quinolone Derivative, was administered in the dose of 800-1200 mg for the mean of 12 days to 24 patients with respiratory tract infection complicating chronic bronchial asthma or chronic obstructive lung disease. Patients with positive sputum culture and bacteria sensitive to pefloxacin were included in the study. Total eradication of the offending microorganisms was achieved in 54% of patients, and partial--in the next 20%. A poor efficacy of pefloxacin against Streptococcus species has been confirmed. In a few cases we have observed the development of resistance of isolated bacteria to pefloxacin during the course of treatment.
M. Ruiz - One of the best experts on this subject based on the ideXlab platform.
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Potentiometric and spectroscopic studies of transition-metal ions complexes with a Quinolone Derivative (cinoxacin). Crystal structures of new Cu(II) and Ni(II) cinoxacin complexes
Journal of Inorganic Biochemistry, 1997Co-Authors: M. Ruiz, R. Ortiz, L. Perelló, Julio Latorre, Juan Server-carrióAbstract:Abstract The interaction of cobalt(II), nickel(II), copper(II), and zinc(II) with Cinoxacin (HCx = 1-ethyl-1,4-dihydro-4-oxo(1,3)dioxolo(4,5-g)cinnoline-3-carboxylic acid), a 4-Quinolone Derivative, has been studied at metal/ligand ratios of 1:1-1:3 by means of pH-metric, spectrophotometric, and ESR methods. The formation constants have been determined and the stereochemistry for the metal ions in the species present in aqueous solutions (at 37 ± 0.1°C and I = 0.1 mol dm −3 NaCl) is discussed. In all the studied systems, complexes with different stoichiometric ratios, in which cinoxacin acts both as neutral and deprotonated ligand, are formed. The anomalous sequence of the stepwise stability constants observed for cobalt(II) and nickel(II) systems suggests changes in stereochemistry when CoCx 2 and NiCx 2 are formed. For zinc(II) this change has to be still more pronounced since a [ZnCx] + species has not been detected. For the Cu(II) system the sequence in the stepwise stability constants indicates the preferential formation of the [CuCx] + monocomplex. The crystal and molecular structure of new Cu(II) and Ni(II) complexes of cinoxacin have been investigated. The metal ion in [Cu(Cx) 2 H 2 O]·3H 2 O is five-coordinated and the complex crystallizes in the triclinic P 1 space group with a = 10.620(1), b = 11.358(1), c = 12.440(2) A , α = 78.25(1), β = 80.24(1), γ = 63.34(1)°, and Z = 2 . The complex [Ni(Cx) 2 -(DMSO) 2 ]·4H 2 O contains six-coordinated Ni(II) and crystallizes in the triclinic P 1 space group with a = 8.866(3), b = 9.141(1), c = 11.580(1) A , α = 69.301(9), β = 82.17(2), γ = 75.86(2)°, and Z = 1 .
Chao-ming Hung - One of the best experts on this subject based on the ideXlab platform.
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cwf 145 a novel synthetic Quinolone Derivative exerts potent antimitotic activity against human prostate cancer rapamycin enhances antimitotic drug induced apoptosis through the inhibition of akt mtor pathway
Chemico-Biological Interactions, 2016Co-Authors: Chao-ming Hung, Chitang HoAbstract:Abstract CWF-145, a synthetic 2-phenyl-4-Quinolone Derivative exerted potent cytotoxicity against prostate cancer. CWF-145 inhibited prostate cancer cell lines PC-3, DU-145 and LNCap. It had a very low IC 50 about 200 nM against castrate-resistant prostate cancer (CRPC) PC-3. We found that CWF-145 had a similar effect to clinical trial antimitotic agents in cancer cells and normal cells. CWF-145 arrested cell cycle at G2/M phase by binding to the β-tubulin at the colchicine-binding site then disrupted microtubule polymerization. Furthermore, the damaged microtubule affected the Akt/mammalian target of rapamycin (mTOR) signaling pathway. Our data showed that CWF-145 activated Akt and mTOR expression to increase emi1 accumulation and inhibit APC. The increased cyclin B1 and securin arrested cell cycle at G2/M phase. Moreover, we showed that Akt activation markedly increased resistance to microtubule-directed agents, including CWF-145, colchicine, and paclitaxel. Interestingly, rapamycin inhibited Akt-mediated therapeutic resistance, indicating that these effects were dependent on mTOR. Taken together, these observations suggest that activation of the Akt/mTOR signaling pathway can promote resistance to chemotherapeutic agents that do not directly target metabolic regulation. These data may provide insight into potentially synergistic combinations of anticancer therapies.
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Inhibition of the insulin-like growth factor 1 receptor by CHM-1 blocks proliferation of glioblastoma multiforme cells.
Chemico-biological interactions, 2015Co-Authors: Ying-chao Lin, Shin-chen Hou, Chao-ming Hung, Jia-ni Lin, Wei-chih Chen, Sheng-chu Kuo, Tzong-der WayAbstract:The insulin-like growth factor-1 receptor (IGF-1R) plays a pivotal role in transformation, growth, and survival of glioblastoma multiforme (GBM) cells, and has emerged as a general and promising target for cancer treatment. In this study, we examined the anti-tumor effects of CHM-1, a synthetic 6,7-methylenedioxy substituted 2-phenyl-4-Quinolone Derivative, on GBM cells in vitro and in vivo. CHM-1 selectively blocked IGF-1R auto-phosphorylation, with an ability to distinguish between IGF-1R and related tyrosine kinase receptors, such as insulin receptor (IR), epidermal growth factor receptor (EGFR), platelet-derived growth factor receptor (PDGFR), and fibroblast growth factor receptor (FGFR). Further investigation revealed that, the phosphorylation of ERK1/2 as well as Akt was inhibited in CHM-1 treated GBM8401 cells possibly through the selective blockage of IGF-1R auto-phosphorylation. Our study also showed that p.o. treatment with the hydrophilic dihydrogen phosphate CHM-1P reduced the tumor volumes of the GBM8401 derived tumors in mouse brain and also prolonged the survival rate. The results provided potential opportunities for effective chemotherapy for GBM.
Chitang Ho - One of the best experts on this subject based on the ideXlab platform.
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cwf 145 a novel synthetic Quinolone Derivative exerts potent antimitotic activity against human prostate cancer rapamycin enhances antimitotic drug induced apoptosis through the inhibition of akt mtor pathway
Chemico-Biological Interactions, 2016Co-Authors: Chao-ming Hung, Chitang HoAbstract:Abstract CWF-145, a synthetic 2-phenyl-4-Quinolone Derivative exerted potent cytotoxicity against prostate cancer. CWF-145 inhibited prostate cancer cell lines PC-3, DU-145 and LNCap. It had a very low IC 50 about 200 nM against castrate-resistant prostate cancer (CRPC) PC-3. We found that CWF-145 had a similar effect to clinical trial antimitotic agents in cancer cells and normal cells. CWF-145 arrested cell cycle at G2/M phase by binding to the β-tubulin at the colchicine-binding site then disrupted microtubule polymerization. Furthermore, the damaged microtubule affected the Akt/mammalian target of rapamycin (mTOR) signaling pathway. Our data showed that CWF-145 activated Akt and mTOR expression to increase emi1 accumulation and inhibit APC. The increased cyclin B1 and securin arrested cell cycle at G2/M phase. Moreover, we showed that Akt activation markedly increased resistance to microtubule-directed agents, including CWF-145, colchicine, and paclitaxel. Interestingly, rapamycin inhibited Akt-mediated therapeutic resistance, indicating that these effects were dependent on mTOR. Taken together, these observations suggest that activation of the Akt/mTOR signaling pathway can promote resistance to chemotherapeutic agents that do not directly target metabolic regulation. These data may provide insight into potentially synergistic combinations of anticancer therapies.
