Magnetic Nano Cobalt Ferrite Catalyzed Synthesis of 4H-Pyrano[3,2-h]quinoline Derivatives under Microwave Irradiation

A microwave irradiated magnetically separable nano cobalt ferrite catalyzed green method for the synthesis of 4-phenyl-4H-pyrano[3,2-h]quinolin-2-amine and 2-amino-4-phenyl-4H-pyrano[3,2-h] quinoline-3-carbonitrile derivatives through cyclization of aromatic aldehyde, acetonitrile/malononitrile and 8-hydoxyquinoline is developed and presented in this paper. The cubic magnetic cobalt ferrite nano particles were synthesized by sol-gel citrate precursor method and characterized by FT-IR, XRD, SEM and TEM techniques and the structures of the synthesized pyranoquinoline derivatives were assigned by IR, MASS and 1H NMR techniques. The reaction is carried out in a domestic microwave oven with a heat-resistant microwave safe glass container with a lid.

Effect of substitution group on dielectric properties of 4H-pyrano [3,2-c] quinoline derivatives thin films

The AC electrical conductivity and dielectrical properties of 2-amino-6-ethyl-5-oxo-4-（3-phenoxyphenyl）-5,6-dihydro-4H-pyrano[3, 2-c]quinoline-3-carbonitrile（Ph-HPQ） and 2-amino-4-（2-chlorophenyl）-6-ethyl-5-oxo-5,6-dihydro-4H-pyrano [3, 2-c] quinoline-3-carbonitrile（Ch-HPQ） thin films were determined in the frequency range of 0.5 k Hz–5 MHz and the temperature range of 290–443 K. The AC electrical conduction of both compounds in thin film form is governed by the correlated barrier hopping（CBH） mechanism. Some parameters such as the barrier height, the maximum barrier height, the density of charges, and the hopping distance were determined as functions of temperature and frequency. The phenoxyphenyl group has a greater influence on those parameters than the chlorophenyl group. The AC activation energies were determined at different frequencies and temperatures. The dielectric behaviors of Ph-HPQ and Ch-HPQ were investigated using the impedance spectroscopy technique. The impedance data are presented in Nyquist diagrams for different temperatures. The Ch-HPQ films have higher impedance than the Ph-HPQ films. The real dielectric constant and dielectric loss show a remarkable dependence on the frequency and temperature. The Ph-HPQ has higher dielectric constants than the Ch-HPQ.

A new fluorescent quinoline derivative toward the acid-responsivity in both solution and solid states

In this article,an acid-responsive luminescent material,1,4-di(quinoline-6-yl)buta-1,3-diyne(DQBD)is designed and synthesized.Upon different pH values,gradual changes of fluorescence colors for DQBD in both solution and solid phases are demonstrated due to the protonation effect.Moreover,such responsive characteristics can also be reversible,suggesting DQBD as a promising fluorescent material with great potential for reusable-and accurate-p H sensors in the future.

Zirconium-mediated Selective Synthesis of Quinoline Derivatives

A series of quinoline derivatives was obtained in high yields by an efficient one-pot reaction of substituted o-diiodobenzenes with azazirconacyelopentadienes, which were conveniently prepared from one internal alkyne and one nitrile mediated by zirconocene. This proposed synthetic method provides a feasible way to the synthesis of large N-heteroeyclic π-conjugated molecules.

Anti-hepatitis C virus potency of a new autophagy inhibitor using human liver slices model

AIM: To evaluate the antiviral potency of a new antihepatitis C virus(HCV) antiviral agent targeting the cellular autophagy machinery. METHODS: Non-infected liver slices, obtained from human liver resection and cut in 350 μm-thick slices(2.7 × 106 cells per slice) were infected with cell culture-grown HCV Con1b/C3 supernatant(multiplicity of infection = 0.1) cultivated for up to ten days. HCV infected slices were treated at day 4 post-infection with GNS-396 for 6 d at different concentrations. HCV replication was evaluated by strand-specific real-time quantitative reverse transcription- polymerase chain reaction. The infectivity titers of supernatants were evaluated by foci formation upon inoculation into naive Huh-7.5.1 cells. The cytotoxic effect of the drugs was evaluated by lactate dehydrogenase leakage assays. RESULTS: The antiviral efficacy of a new antiviral drug, GNS-396, an autophagy inhibitor, on HCV infection of adult human liver slices was evidenced in a dosedependent manner. At day 6 post-treatment, GNS-396 EC50 was 158 nmol/L without cytotoxic effect(compared to hydroxychloroquine EC50 = 1.17 μmol/L).CONCLUSION: Our results demonstrated that our ex vivo model is efficient for evaluation the potency of autophagy inhibitors, in particular a new quinoline derivative GNS-396 as antiviral could inhibit HCV infection in a dosedependent manner without cytotoxic effect.

Synthesis and Crystal Structure of a Novel Bis(chlorido)-bridged One-dimensional Chain-like Copper(Ⅱ) Polymer

A copper（Ⅱ） complex [LCu2Cl4]n was synthesized by a new bis-Schiff base ligand containing quinoline unit, 1,4-bis[2-（4-fluorophenyl）iminomethyl-8-quinolinoxy]butane（L）. X-ray crystal structure shows that it is a binuclear complex, and the crystal belongs to the triclinic system, space group P1, with a = 9.387（2）, b = 9.968（2）, c = 10.291（2） ？, α = 87.532（3）, β = 63.762（2）, γ = 86.628（3）o, V = 862.1（3） ？^3, Z = 1, Dc = 1.640 Mg/m^3, F（000） = 428, R = 0.0416 and wR = 0.1141. Each Cu（Ⅱ） metal ion coordinates with a quinoline N atom, an imine N atom, an ether oxygen atom and three chlorides, forming a distorted six-coordinated octahedronal structure. Each copper（Ⅱ） complexation unit links with one of the adjacent ligand copper complexation units through the chlorido bridging groups, thus generating an infinite one-dimensional chain structure. Such 1D chains further construct a 2D network structure by π-π stacking interactions.

Novel thieno[2,3-b]quinoline-procaine hybrid molecules:A new class of allosteric SHP-1 activators evolved from PTP1B inhibitors

Small molecule activators could equally provide powerful tools as inhibitors do for interrogating cellular signal transduction.However,targeted protein activation is chemically challenging.Developing activators against Src homology region 2 domain-containing phosphatase-1(SHP-1)to block STAT3 pathway represents a promising strategy for DLBCL therapy.Here we reported a new class of thieno[2,3-b]quinolineprocaine hybrid molecules as SHP-1 allosteric activators.The representative hybrid compound 3b displayed SHP-1 activating effect with EC50 of 5.48±0.28μmol/L.Further investigations confirmed that 3b allosterically interacted with SHP-1,switched it from close to open conformation,blocked SHP-1/p-STAT3 pathway,induced apoptosis and inhibited ABC-DLBCL cell proliferation in vitro,and delayed tumor growth in the xenograft model of SU-DHL-2.Overall,this work offered a novel paradigm to develop SHP-1 allosteric activators through chemical space evolution of PTPs inhibitors,and firstly validated the therapeutic strategy that directly activating SHP-1 alone could be a potential therapy against ABC-DLBCL via blocking STAT3 pathway.

Design, Synthesis and Biological Evaluation of Novel α-Acyloxycarboxamide-Based Derivatives as c-Met Inhibitors

Dysregulated HGF/c-Met signalling has been associated with many human cancers,poor clinical outcomes,and even resistance acquisition to some approved targeted therapies.As such,c-Met kinase has emerged as an attractive target for anticancer drug discovery.