- METHOD FOR PRODUCING 3-METHYL-2-THIOPHENECARBOXYLIC ACID
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A method for producing 3-methyl-2-thiophenecarboxylic acid is provided. A method for producing 3-methyl-2-thiophenecarboxylic acid, which comprises reacting a compound represented by the formula (I): (wherein X is a chlorine atom or a bromine atom) with magnesium in the presence of an alkyl halide to give a Grignard reagent represented by the formula (II): (wherein X is the same as defined above), reacting the Grignard reagent of the formula (II) with carbon dioxide, and acidifying the reaction product.
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- Synthesis of N-(Methoxycarbonylthienylmethyl)thioureas and evaluation of their interaction with inducible and neuronal nitric oxide synthase
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Two isomeric N-(memoxycarbonylmienylmemyl)mioureas were synthesised by a sequence of radical bromination of methylthiophenecarboxylic esters, substitution with trifluoroacetamide anion, deprotection, formation of the corresponding isothiocyanates and addition of ammonia. The interaction of these new thiophene-based thioureas with inducible and neuronal nitric oxide synthase was evaluauted. These novel thienylmethyl- thioureas stimulated the activity of inducible Nitric Oxide Synthase (iNOS).
- Suaifan, Ghadeer A.R.Y.,Goodyer, Claire L.M.,Threadgill, Michael D.
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experimental part
p. 3121 - 3134
(2010/09/04)
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- RAF KINASE INHIBITORS
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Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.
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Page/Page column 20-21
(2008/12/06)
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- TRICYCLIC DERIVATIVES OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, THEIR PREPARATIONS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
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The present invention relates to tricyclic derivatives or pharmaceutically acceptable salts thereof, their preparations and pharmaceutical compositions containing them. More precisely, the present invention relates to tricyclic derivatives as colchicine derivatives, pharmaceutically acceptable salts thereof, their preparations and pharmaceutical compositions containing them. Tricyclic derivatives of the present invention show very powerful cytotoxicity to cancer cell lines but were much less toxic than colchicine or taxol, confirmed through animal toxicity test. Tricyclic derivatives of the invention also decrease the volume and weight of a tumor and have a strong angiogenesis inhibiting activity in HUVEC cells. Thus, tricyclic derivatives of the present invention can effectively be used as an anticancer agent, anti-proliferation agent and an angiogenesis inhibitor.
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- Substituted 3-aryl-5-aryl-[1,2,4]-oxadiazoles and analogs as activators of caspases and inducers of apoptosis and the use thereof
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The present invention is directed to substituted 3-aryl-5-aryl-[1,2,4]-oxadiazoles and analogs thereof, represented by the Formula I: wherein Ar1, Ar3, A, B and D are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
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- Generation of thiols by biotransformation of cysteine-aldehyde conjugates with baker's yeast
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Baker's yeast was shown to catalyze the transformation of cysteine-furfural conjugate into 2-furfurylthiol. The biotransformation's yield and kinetics were influenced by the reaction parameters such as pH, incubation mode (aerobic and anaerobic), and substrate concentration. 2-Furfurylthiol was obtained in an optimal 37% yield when cysteine-furfural conjugate at a 20 mM concentration was anaerobically incubated with whole cell baker's yeast at pH 8.0 and 30 °C. Similarly to 2-furfurylthiol, 5-methyl-2-furfurylthiol (11%), benzylthiol (8%), 2-thiophenemethanethiol (22%), 3-methyl-2-thiophenemethanethiol (3%), and 2-pyrrolemethanethiol (6%) were obtained from the corresponding cysteine-aldehyde conjugates by incubation with baker's yeast. This work indicates the versatile bioconversion capacity of baker's yeast for the generation of thiols from cysteine-aldehyde conjugates. Thanks to its food-grade character, baker's yeast provides a biochemical tool to produce thiols, which can be used as flavorings in foods and beverages.
- Huynh-Ba, Tuong,Matthey-Doret, Walter,Fay, Laurent B.,Rhlid, Rachid Bel
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p. 3629 - 3635
(2007/10/03)
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- Inhibition of p38 kinase activity by aryl ureas
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This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases other than cancer and proteolytic enzyme mediated diseases other than cancer, and pharmaceutical compositions for use in such therapy.
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- Inhibition of raf kinase activity using aryl ureas
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Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.
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- Regioselective α-and β-Metallations of Thiophene Derivatives Bearing the 4,4-Dimethyloxazolin-2-yl Group. Application of the Method to Syntheses of 2,3- and 2,5-Disubstituted Thiophene Derivatives
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The effects of change of solvent, metallating agent, reaction time and temperature, and of the presence or absence of agents capable of complex formation with either the lithium cation or the oxazoline moiety, on the lithiation of 4,4-dimethyl-2-(2-thienyl)oxazoline are explored.Conditions are thereby established for high-yielding syntheses of the 3- and 5-lithio-intermediates and for control of regioselectivity of metallation.The nucleophilicity of 3-lithio-intermediate is profoundly solvent dependent, and appropriate conditions for reaction of both 3- and 5-lithiated species with a wide variety of electrophiles are presented.Syntheses of a range of 2,3- and 2,5-disubstituted thiophene derivatives have thereby been achieved, utilising, in addition, a new method for the transformation of oxazolino into carboxy functionality.The balance between basicity and nucleophilicity of the 3-lithio-intermediate in its reaction with - and -acetone is shown to be sensitive to isotope effects.
- Carpenter, Andrew J.,Chadwick, Derek J.
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p. 173 - 182
(2007/10/02)
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- HIGH-YIELD SYNTHESES OF 2,3-DISUBSTITUTED FURANS AND THIOPHENES
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The course of lithiation of furan- and thiophene-2-carboxylic acids is critically dependent on the identity of the lithium base allowing high-yielding syntheses of 2,3- and 2,5-disubstituted thiophenenes: the proposed use of a trimethylsilyl blocking group to control metallation in the furan acid provides a useful route to 2,3-disubstituted furans.
- Carpenter, Andrew J.,Chadwick, Derek J
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p. 1777 - 1780
(2007/10/02)
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- CARBOXYLATION OF 1,3-DIMETHYLURACIL AND THIOPHENES WITH CARBON MONOXIDE AND PALLADIUM(II) ACETATE IN THE PRESENCE OF SODIUM PEROXODISULFATE
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Treatments of 1,3-dimethyluracil and of thiophenes with palladium(II) acetate and sodium peroxodisulfate under a carbon monoxide atmosphere gave 1,3-dimethyluracil-5-carboxylic acid and the corresponding thiophene-2-carboxylic acids, respectively.
- Itahara, Toshio
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p. 127 - 128
(2007/10/02)
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- Dianions of Methylated Thiophene-2-carboxylic Acids: Their Formation and Reactivity
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Methylated thiophene-2-carboxylic acids can be readily homologated by treatment with LDA (2 equiv) followed by the addition of carbon-containing electrophiles.
- Gould, Norman P.,Lee, Ta-Jyh
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p. 4528 - 4530
(2007/10/02)
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- Dibenz[b,e]oxepinalkanoic acids as nonsteroidal antiinflammatory agents. 2. Dihydro 10 oxofuro and thieno[3,2 c] [1]benzoxepin 8 acetic acids
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4,10 Dihydro-10-oxofuro[3,2-c][1]benzoxepin-8-acetic acid and 4,10-dihydro-10-oxothieno[3,2-c][1]benzoxepin-8-acetic acid were evaluated in the carrageenan paw edema assay with the thieno analogue being ten times more active than the furano compound and 1.3 times more active than indomethacin. The therapeutic ratio (antiinflammatory activity/gastric irritation liability) of the thieno analogue was 25 times that of indomethacin.
- Aultz,McFadden,Lassman
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p. 456 - 458
(2007/10/11)
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