478374-91-3Relevant academic research and scientific papers
Synthesis and antiproliferative activity of 8-hydroxyquinoline derivatives containing a 1,2,3-triazole moiety
De O. Freitas, Luiza B.,Borgati, Thiago F.,De Freitas, Rossimiriam P.,Ruiz, Ana L. T. G.,Marchetti, Gabriela M.,De Carvalho, Joo E.,Da Cunha, Elaine F. F.,Ramalho, Teodorico C.,Alves, Rosemeire B.
, p. 595 - 604 (2014)
Twelve novel 8-hydroxyquinoline derivatives were synthesized with good yields by performing coppercatalyzed Huisgen 1,3-dipolar cycloaddition ("click" reaction) between an 8-O-alkylated-quinoline containing a terminal alkyne and various aromatic or protected sugar azides. These compounds were evaluated in vitro for their antiproliferative activity on various cancer cell types. Protected sugar derivative 16 was the most active compound in the series, exhibiting potent antiproliferative activity and high selectivity toward ovarian cancer cells (OVCAR-03, GI50 -1); this derivative was more active than the reference drug doxorubicin (OVCAR-03, GI50 = 0.43 μg mL-1). In structureeactivity relationship (SAR) studies, the physico-chemical parameters of the compounds were evaluated and docking calculations were performed for the a-glucosidase active site to predict the possible mechanism of action of this series of compounds.
Synthesis and phytotoxic activity of 1,2,3-triazole derivatives
Borgati, Thiago F.,Alves, Rosemeire B.,Teixeira, Ro?bson R.,De Freitas, Rossimiriam P.,Perdiga?o, Thays G.,Da Silva, Silma F.,Dos Santos, Aline Aparecida,De Jesu?s O. Bastidas, Alberto
, p. 953 - 961 (2013/08/23)
Thirteen triazole derivatives bearing halogenated benzyl substituents were synthesized using the Cu-catalyzed azide-alkyne cycloaddition (CuAAC),a leading example of the click chemistry approach,as the key step. The biological activity of the compounds was evaluated,and it was found that these compounds interfere with the germination and radicle growth (shoots and roots) of two dicotyledonous species,Lactuca sativa and Cucumis sativus,and one monocotyledonous species,Allium cepa. The compounds showed predominantly inhibitory activity related to the evaluated species mainly at the concentration of 10-4 mol L-1. Some of them presented inhibitory activity comparable to 2,4-D (2,4-dichlorophenoxyacetic acid),used as positive control.
SUBSTITUTED ISOXAZOLINE DERIVATIVES
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, (2011/10/19)
This invention recites substituted isoxazoline derivatives of Formula (1) or a veterinarily acceptable salt thereof, with parasiticidal activity, compositions thereof, and their use as a parasiticide in animals or birds where R1a, R1b/sup
ISOMERIC PURINONES AND 1H-IMIDAZOPYRIDINONES AS PKC-THETA INHIBITORS
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Page/Page column 39, (2009/06/27)
A chemical genus of purinones and 1H-imidazopyridinones, which are useful as PKCθ inhibitors, and their methods of use are disclosed. The genus is represented by the Formula (I).
CARBOXYLIC ACID DERIVATIVE AND MEDICINE COMPRISING SALT OR ESTER OF THE SAME
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Page 86, (2010/02/05)
The present invention provides novel carboxylic acid derivatives useful as an insulin sensitizer, a salt thereof or a hydrate of them, and a medicament comprising the derivative as the active ingredient. Specifically, it provides a carboxylic acid derivative represented by the following formula: (wherein L represents a single bond, or a C1 to C6 alkylene group, a C2 to C6 alkenylene group or a C2 to C6 alkynylene group, each of which may have one or more substituent groups; M represents a single bond, or a C1 to C6 alkylene group, a C2 to C6 alkenylene group or a C2 to C6 alkynylene group, each of which may have one or more substituent groups; T represents a single bond, or a C1 to C3 alkylene group, a C2 to C3 alkenylene group or a C2 to C3 alkynylene group, each of which may have one or more substituent groups; W represents a carboxyl group; X represents a single bond, an oxygen atom, or a group represented by the various substituent groups including -NRX1CQ1O- (wherein Q1 represents an oxygen atom or a sulfur atom; RX1 represents a hydrogen atom, a cyano group, a formyl group, or various groups including a C1 to C6 alkyl group and a C1 to C6 hydroxyalkyl group, each of which may have one or more substituent groups) , ONRX1CQ1-, -NRX1CQ1-, -CQ1NRX1-, -NRX1aCQ1NRX1b-, -Q2SO2- and -SO2Q2-; Y represents a 5 to 14-membered aromatic group which may have one or more substituent groups and one or more hetero atoms, or a C3 to C7 alicyclic hydrocarbon group; and the rings Z and U may be the same as or different from each other and each represents a 5 to 14-membered aromatic group which may have 1 to 4 substituent groups and one or more hetero atoms, and the ring may be partially saturated.), a salt thereof, an ester thereof or a hydrate of them.
