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5-Fluorouracil derivatives of this invention are represented by the general formula: STR1 wherein R indicates an alkylene group having 1-8 carbon atoms, A indicates an atomic group of –NH– and –CO–, n is 0 or 1, and Y indicates an alkyl group having 1-10 carbon atoms, an aryl group, a heteroaryl group, a pyridinium ion having a halogen as a pair ion or an isocyanate group. These derivatives are useful as anticancer medicines and intermediates therefor. These derivatives are produced by six specified methods of this invention. A representative method is a process which comprises reacting 5-fluorouracil and an isocyanate represented by a general formula: wherein R, A, n and Y are the same as those indicated in the formula (I).

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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

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The first isolation and structure elucidation of four sulfur-containing indole phytoalexins from Chinese cabbage inoculated with Pseudomonas cichorii are described.

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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

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To explore the chemical composition of root exudates of the model plant Arabidopsis thaliana a workflow for nontargeted metabolite profiling of the semipolar fraction of root exudates was developed. It comprises hydroponic plant cultivation and sampling of root exudates under sterile conditions, sample preparation by solid-phase extraction and analysis by reversed-phase UPLC/ESI-QTOFMS. Following the established workflow, root exudates of six-week-old plants were profiled and a set of reproducibly occurring molecular features was compiled. To structurally elucidate the corresponding metabolites, accurate mass tandem mass spectrometry and on-line hydrogen/deuterium exchange were applied. Currently, a total of 103 compounds were detected and annotated by elemental composition of which more than 90 were structurally characterized or classified. Among them, 42 compounds were rigorously identified using an authenticated standard. The compounds identified so far include nucleosides, deoxynucleosides, aromatic amino acids, anabolites and catabolites of glucosinolates, dipeptides, indolics, salicylic and jasmonic acid catabolites, coumarins, mono-, di- and trilignols, hydroxycinnamic acid derivatives and oxylipins and exemplify the high chemical diversity of plant root exudates.

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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

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The reactant in an enzyme-catalyzed reaction is called a substrate. Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction.I hope my blog about 22259-53-6 is helpful to your research. Electric Literature of 22259-53-6

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The present invention concerns 2-amino-pyridin-3-yl carboxamide and 3-amino-pyrazin-2-yl carboxamide derivatives of formula (I): (I) or a pharmaceutically acceptable salt thereof, wherein: ? A is N or C-H, ? Y is 0, S or one of the following groups : sulfoxide (-S(O)-), sulfone (- S(0)2-) or N (R3) with R3being H, or an optionally substituted alkyl, acyl, alkenyl, alkynyl, cycloalkyl, aralkyl, aryl or heteroaryl, ? R1 is H or an optionally substituted alkyl, acyl, alkenyl, alkynyl, cycloalkyl, aralkyl, aryl or heteroaryl, or when Y is NR3, R1 and R3 are together included into an optionally substituted 4 to 7-membered heterocycle or 8 to 10-membered heterobicycle, and ? R2 is any of the optionally substituted following groups: alkyl, acyl, alkenyl, alkynyl, cycloalkyl, aralkyl, aryl, heteroaryl-alkyl or heteroaryl; for use as polo-like kinase 2 inhibitors for the treatment of cancer; as well as pharmaceutical compositions containing such a compound and processes to prepare such a compound.

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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

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Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 22259-53-6, molcular formula is C9H10N2, introducing its new discovery. Quality Control of: (1H-Indol-3-yl)methanamine

Synthesis of isochromanones and isoquinolones comprising a quaternary center with high diastereoselectivity was realized via a AuCl3 catalyzed tandem intramolecular exo-dig heterocyclization/enol isomerization/Claisen rearrangement sequence in excellent yields. The reaction is general and amenable for the synthesis of structurally diverse analogues.

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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

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Substituted trichloroacetamidine derivatives are prepared by treating an appropriately substituted imidate with ammonia. The imidate intermediates are prepared by treating an appropriately substituted amine with an imidating reagent.

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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

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Driving factors in amiloride recognition of HIV RNA targets

Noncoding RNAs are increasingly promising drug targets yet ligand design is hindered by a paucity of methods that reveal driving factors in selective small molecule:RNA interactions, particularly given the difficulties of high-resolution structural characterization. HIV RNAs are excellent model systems for method development given their targeting history, known structure-function relationships, and the unmet need for more effective treatments. Herein we report a strategy combining synthetic diversification, profiling against multiple RNA targets, and predictive cheminformatic analysis to identify driving factors for selectivity and affinity of small molecules for distinct HIV RNA targets. Using this strategy, we discovered improved ligands for multiple targets and the first ligands for ESSV, an exonic splicing silencer critical to replication. Computational analysis revealed guiding principles for future designs and a predictive cheminformatics model of small molecule:RNA binding. These methods are expected to facilitate progress toward selective targeting of disease-causing RNAs.

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Reference£º
Indole alkaloid derivatives as building blocks of natural products from?Bacillus thuringiensis?and?Bacillus velezensis?and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

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AN INTRAMOLECULAR PHOTOCYCLIZATION TO FORM THE AZEPINO<3,4,5-cd>INDOLE SYSTEM

Azepino<3,4,5-cd>indoles 5a and 5b are formed in good yield via the intramolecular photocyclization of N-chloroacetyl-3-aminomethylindoles.

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Reference£º
Indole alkaloid derivatives as building blocks of natural products from?Bacillus thuringiensis?and?Bacillus velezensis?and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles