Discovery of 1081-17-0

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ALKALOIDS FROM Papaver litwinowii FEDDE ex BORNM.

From Papaver litwinowii FEDDE ex BORNM. aporheine ((+)-roemerine) was isolated as the dominant alkaloid in addition to minor alkaloids aporheine methohydroxide, corytuberine, hordenine, (-)-mecambrine, cryptopine, protopine and coptisine.The presence of small amounts of allocryptopine, corydine, isocorydine, scoulerine, corysamine and papaverrubine A, C, D and traces of E(?) was also proved.Corytuberine was now isolated from P. dubium L. as well.

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Preparation and Characterization of Hetero-bifunctional Cross-linking Reagents for Protein Modifications

Ten aromatic and aliphatic cross-linking reagents of hetero-bifunctional type were synthesized as part of a search for useful reagents of this type.All of the reagents possess two selectively reactive groups a maleimide group which can combine with a thiol group via its double bond and an N-Hydroxysuccinimidyl ester (one of the most hydrophilic active esters), which can react with an ammmine group.It was found that the active esters of the reagents tested were mostly more reactive with lysine than with leucine, and acylated amino acids more rapidly at pH 8.0 than at pH 7.0.It was also found that the stability of the maleimide group in the compounds tested depends largely upon the pH of the buffer used.The most stable pH was 5.0-6.0.To use one of the present compounds as a cross-linker, the crystalline reagent should be dissolved in tetrahydrofuran of dioxane and the solution used for cross-linking.The acylation step should be carried out first with thiol addition to the maleimide group as the second step.The optimum pH of the buffer used for the first step is slightly basic.The reaction time should be limited to less than 1 hr.When the first step is over, the pH of the reaction mixture should be changed to 5.0-6.0.Keywords—cross-linker; hetero-bifunctional reagent; reactivity of N-hydroxy-succinimidyl ester; stability of maleimide residue; N-(maleimidobenzoyloxy)succinimide derivative; N-(maleimidoalkyloxy)succinimide derivative

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ENTACAPONE-DERIVATIVES

Pharmaceutical composition comprising one or more entacapone derivatives and one or more pharmaceutically acceptable carriers, a process for producing the pharmaceutical composition, specific entacapone derivatives, a process for the preparation of entacapone derivatives, and the use of the entacapone derivatives for the preparation of a medicament.

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Synthesis of cytotoxic pyrroloquinazolinoquinoline alkaloid luotonin A

A convenient synthesis of cytotoxic pyrroloquinazolinoquinoline alkaloid, luotonin A (1), was achieved in 3 steps; (i) reaction of anthranilic acid with O-methylbutyrolactim to deoxyvasicinone, (ii) oxidation of deoxyvasicinone, and (iii) formation of luotonin A by the reaction of vasicinone with anthranyl aidehyde.

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Aryloxymaleimides for cysteine modification, disulfide bridging and the dual functionalization of disulfide bonds

Tuning the properties of maleimide reagents holds significant promise in expanding the toolbox of available methods for bioconjugation. Herein we describe aryloxymaleimides which represent ‘next generation maleimides’ of attenuated reactivity, and demonstrate their ability to enable new methods for protein modification at disulfide bonds.

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Propionic Acid Derivatives and Methods of Use Thereof

Provided herein are compounds and pharmaceutical compositions of formula I where R1, R2, R3, R4, R5 and R6 are as described herein. Also provided pharmaceutically acceptable salts or stereoisomers of these compounds. In addition methods are provided for inhibiting the binding of an integrin to treat various pathophysiological conditions.

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Rhodium(III)-Catalyzed C-H Alkenylation: Access to Maleimide-Decorated Tryptophan and Tryptophan-Containing Peptides

Maleimide is widely applied in many fields, especially in antibody-drug conjugations and peptide drugs. Herein, we develop a strategy for the C-H alkenylation of tryptophan and tryptophan-containing peptides, providing a synthetic route of decorating maleimide on peptides. The method has a high tolerance of functional groups and protecting groups. Furthermore, this method was applied to prepare peptide conjugation with molecules such as drugs and fluorescence probes. Moreover, macrocyclic peptides were obtained via this reaction.

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In heterogeneous catalysis, the catalyst is in a different phase from the reactants. Application In Synthesis of 1-(4-Methoxyphenyl)-1H-pyrrole-2,5-dione, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 1081-17-0, name is 1-(4-Methoxyphenyl)-1H-pyrrole-2,5-dione. In an article£¬Which mentioned a new discovery about 1081-17-0

ALKALOIDS OF THE TWO Hypecoum L. SPECIES

Alkaloids from Hypecoum procumbens L. and H. leptocarpum HOOK.F. et THOMS. were investigated.Protopine was the dominant alkaloid in both species.From H. procumbens chelerythrine and corydine were newly isolated in addition to the earlier detected alkaloids allocryptopine, sanguinarine, coptisine, and isocorydine.From H. leptocarpum allocryptopine, isocorydine, and corydine were isolated for the first time, in addition to the earlier described alkaloids protopine, sanguinarine, chelerythrine, and coptisine.Cryptopine was detected chromatographically.From the fraction of strongly polar alkaloids of both species magnoflorine, (-)-trans-N-methylstylopinium hydroxide, and in small amounts a new secoberbine alkaloid of oxohypecorinine structure, procumbine (I), and two further alkaloids of unresolved structure were isolated in the form of iodides.

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High diastereoselectivity induced by intermolecular hydrogen bonding in [3?+?2] cycloaddition reaction: experimental and computational mechanistic approaches

A diastereoselective [3?+?2] cycloaddition of N-aryl substituted maleimides with N,alpha-diphenyl nitrone possessing 11-hydroxyundecyloxy as a flexible substituent was performed. Experimental and comprehensive mechanistic density functional theory studies reveals that intermolecular H-bonding and steric repulsive interaction predominate exo-Z and exo-E cycloaddition transition states, respectively. The reaction proceeded smoothly depending on the reactants and gave a good yield of (syn) cis-isoxazolidine or (anti) trans-isoxazolidine as a single diastereomer.

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ANTIBODY CONJUGATES COMPRISING TOLL-LIKE RECEPTOR AGONIST

Provided herein are antibody conjugates comprising toll-like receptor agonists and the use of such conjugates for the treatment of cancer. In some embodiments, the conjugates comprise anti-HER2 antibodies.

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