608-34-4Relevant articles and documents
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Pitha
, p. 903 (1970)
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Pyrimidinedione derivative capable of inhibiting monocarboxylate transporter
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Paragraph 0192; 0193, (2019/03/26)
The invention relates to a pyrimidinedione derivative capable of inhibiting a monocarboxylate transporter, the pyrimidinedione derivative is a formula (I) compound and/or a pharmaceutically acceptablesalt thereof, and/or a stereoisomer thereof, and/or a solvate thereof, the compound has the effect of inhibiting the activity of the monocarboxylate transporter, and also comprises a pharmaceutical composition containing the formula (I) compound and the use of the pharmaceutical composition in treatment.
Discovery of a new class of highly potent inhibitors of acid ceramidase: Synthesis and structure-activity relationship (SAR)
Pizzirani, Daniela,Pagliuca, Chiara,Realini, Natalia,Branduardi, Davide,Bottegoni, Giovanni,Mor, Marco,Bertozzi, Fabio,Scarpelli, Rita,Piomelli, Daniele,Bandiera, Tiziano
supporting information, p. 3518 - 3530 (2013/06/27)
Acid ceramidase (AC) is an intracellular cysteine amidase that catalyzes the hydrolysis of the lipid messenger ceramide. By regulating ceramide levels in cells, AC may contribute to the regulation of cancer cell proliferation and senescence and to the response to cancer therapy. We recently identified the antitumoral agent carmofur (4a) as the first nanomolar inhibitor of intracellular AC activity (rat AC, IC50 = 0.029 μM). In the present work, we expanded our initial structure-activity relationship (SAR) studies around 4a by synthesizing and testing a series of 2,4-dioxopyrimidine-1- carboxamides. Our investigations provided a first elucidation of the structural features of uracil derivatives that are critical for AC inhibition and led us to identify the first single-digit nanomolar inhibitors of this enzyme. The present results confirm that substituted 2,4-dioxopyrimidine-1-carboxamides are a novel class of potent inhibitors of AC. Selected compounds of this class may represent useful probes to further characterize the functional roles of AC.
PROCESS FOR STRAIGHTENING KERATIN FIBRES WITH A HEATING MEANS AND DENATURING AGENTS
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, (2010/03/02)
The invention relates to a process for straightening keratin fibres, comprising: (i) a step in which a straightening composition containing at least two denaturing agents is applied to the keratin fibres, (ii) a step in which the temperature of the keratin fibres is raised, using a heating means, to a temperature of between 110 and 250° C.