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Synthesis and evaluation of 5-substituted 9-hydroxypyrrolo[3,4-c]carbazole- 1,3(2H,6H)-diones as check point 1 kinase inhibitors

The structure-activity relationship (SAR) of 5-substituted pyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione derivatives 5 was investigated for their potential as Chk1 inhibitors for possible chemo- and radio-potentiators in anticancer chemotherapies. In silico virtual screening helped to optimize the substituent on the phenyl ring, and led to identification of the m-carbamoyl group among the 117 analogues tested. Further optimization studies focusing on the docking model of 15 in the active site of Chk1 revealed that 32b (IC 50 = 2.8 nM) was a more potent inhibitor than UNC-01.

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Pyrroline – Wikipedia,
1-Pyrroline | C4H7N – PubChem

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High pseduo-stoke’s shift of a naphthalene-bisindolylmaleimide dye

An energy transfer cassette was reported with energy donor and acceptor incorporated in one molecular. The two units (naphthalene and bisindolylmaleimide) were connected by covalent single bond. The intramolecular repulsion twisted the molecular conformation, thereby forcing the two units act as independent chromophores. Upon photoexcitation (lambda = 280 nm), bright emission peak was observed around 583 nm. The intramolecular cascade energy transfer from the naphthalene moiety to the bisindolylmaleimide framework is efficient and the efficiency is estimated to be 86%, providing large pseudo-Stoke’s shift (303 nm). At such a short separation, the orbital overlap interaction was completely isolated between chromophoric units. Computational study was carried out based on DFT. Further analysis of optimized structure and FMOs supports the efficient energy transfer in NBM. Favorable photophysical properties, such as efficient energy transfer, strong emission, and large Stoke’s shift make it an attractive functional dye.

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Application of 1122-10-7, 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, 1122-10-7, molcular formula is C4HBr2NO2, introducing its new discovery.

Four new bioactive pyrrole-derived alkaloids from the marine sponge Axinella brevistyla

Four new alkaloids (1-4) were isolated from the marine sponge Axinella brevistyla, and their structures were determined on the basis of spectroscopic analysis. The alkaloids 1-4 were antifungal against the yeast Saccharomyces cerevisiae at <1.0, <1.0, 30, and 100 mug/disk, respectively. Compounds 1-3 also exhibited cytotoxicity against L1210 cells with IC50 values of 1.1, 0.66, and 2.5 mug/mL, respectively. The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 1122-10-7 is helpful to your research. Application of 1122-10-7

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Pyrroline – Wikipedia,
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Fluorescence and chemiluminescence properties of indolylmaleimides: Experimental and theoretical studies

Various indolylmaleimides (IMs) were synthesized, and their fluorescence (FL) and chemiluminescence (CL) were measured. The substitution at the 2-position of the indole ring and the 3- or 4-position of the maleimide moiety caused an obvious change in the FL and CL of the IMs. An almost on-off switching of the FL of the IMs was observed. The intramolecular charge transfer from the indole moiety to the maleimide moiety occurred in 3-(1H-3-indolyl)-2,5-dihydro- 1H-2,5-pyrroledione. In the FL of the IMs, CASPT2 calculations showed deprotonation of the NH group of the indole ring and the maleimide moiety at the excited state. The CC bond in the maleimide moiety was needed for strong CL in the IMs without substitution at the 2-position of the indole ring. The relationships between the FL or CL properties and the structures of the IMs were clarified. These results provide significant information on the rational design of IMs as FL and CL probes.

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Pyrroline – Wikipedia,
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Scalable preparation of stable and reusable silica supported palladium nanoparticles as catalysts for N-alkylation of amines with alcohols

The development of nanoparticles-based heterogeneous catalysts continues to be of scientific and industrial interest for the advancement of sustainable chemical processes. Notably, up-scaling the production of catalysts to sustain unique structural features, activities and selectivities is highly important and remains challenging. Herein, we report the expedient synthesis of Pd-nanoparticles as amination catalysts by the reduction of simple palladium salt on commercial silica using molecular hydrogen. The resulting Pd-nanoparticles constitute stable and reusable catalysts for the synthesis of various N-alkyl amines using borrowing hydrogen technology without the use of any base or additive. By applying this Pd-based catalyst, functionalized and structurally diverse N-alkylated amines as well as some selected drug molecules were synthesized in good to excellent yields. Practical and synthetic utility of this Pd-based amination protocol has been demonstrated by upscaling catalyst preparation and amination reactions to several grams-scales as well as recycling of catalyst. Noteworthy, this Pd-catalyst preparation has been up-scaled to kilogram scale and catalysts prepared in both small (1 g) and large-scale (kg) exhibited similar structural features and activity.

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Pyrroline – Wikipedia,
1-Pyrroline | C4H7N – PubChem

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Visible-Light-Triggered Activation of a Protein Kinase Inhibitor

A photoresponsive small molecule undergoes a ring-opening reaction when exposed to visible light and becomes an active inhibitor of the enzyme protein kinase C. This ?turning on? of enzyme inhibition with light puts control into the hands of the user, creating the opportunity to regulate when and where enzyme catalysis takes place.

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LYSOSOME-CLEAVABLE LINKER

The present invention relates to a linker for forming conjugates of a protein or peptide with a therapeutically active agent and which comprise a thiomaleamic acid moiety that is susceptible to cleavage under the pH conditions prevalent in the lysosome.

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Pyrroline – Wikipedia,
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Synthesis and antimicrobial activity of 3,4-bis(arylthio)maleimides

A series of 3,4-bis(arylthio)maleimides were synthesized and their antimicrobial activity was evaluated against Gram-positive and Gram-negative bacteria, including multidrug resistant (MDR) strains and some fungi. Most compounds turned out to be highly active, activity being dependent on substituents on phenyl rings.

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Pyrroline – Wikipedia,
1-Pyrroline | C4H7N – PubChem

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Synthesis of bis(indolylmaleimide) macrocycles

The synthesis of a novel class of macrocyclic bis(indolylmaleimides) is reported. The key step involves the intermolecular connection of 2,2′-bridged indoles with 3,4-dibromo-2,5-dihydro-1H-2,5-pyrroledione (dibromomaleimide) derivatives. The bis(indolylmaleimides) afforded by this method were further processed by intramolecular nucleophilic substitution of the remaining bromo substituents forming flexible N-substituted macrocycles (9a-9j, 10a-10e) and, by connecting both maleimides, semi rigid macrocycles (7a-7xx).

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Reduction-responsive dithiomaleimide-based nanomedicine with high drug loading and FRET-indicated drug release

Dithiomaleimide-based camptothecin-containing nanoparticles are designed to have exceptionally high drug loading and are capable of reduction-responsive, FRET-indicated drug release.

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Pyrroline – Wikipedia,
1-Pyrroline | C4H7N – PubChem