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PMR SPECTRA AND cis-trans ISOMERISM OF 2-METHYLENEPYRROLIDINE AND 2-METHYLENETETRAHYDROFURAN DERIVATIVES

A number of secondary enamines and cyclic enol ethers (2-methylenetetrahydrofuran derivatives) were synthesized by the reaction of O-methylbutyrolactim and 2,2-diethoxytetrahydrofuran, respectively, with compounds that have an active methylene link.The absence of reversible cis-trans isomerization was established in a study of the PMR spectra of these compounds.The configuration of the secondary enamines is determined by the possibility of the formation of a strong intramolecular hydrogen bond between the carbonyl-containing substituent and the NH group.In the case of the cyclic enol ethers it was shown that the energy barrier to cis-trans isomerization is greater than 25 kcal/mole and that, as a consequence of this, the geometrical isomers can be separated preparatively.

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Pyrroline – Wikipedia,
1-Pyrroline | C4H7N – PubChem

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Electric Literature of 69778-83-2, A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 69778-83-2, Name is 4-Methoxy-1H-pyrrol-2(5H)-one, molecular formula is C5H7NO2. In a Article£¬once mentioned of 69778-83-2

A scalable process for the synthesis of the Bcl inhibitor obatoclax

Recently we created the novel indolylprodigiosin derivative 2 (obatodax) and demonstrated its ability to antagonize multiple members of the B-cell lymphoma (Bd) family of antiapoptotic proteins. The compound has shown potent anticancer activity in several animal tumor models. Obatodax is now in Phase 1b and 2 clinical trials directed against multiple hematologic and solid tumor malignancies. To support its clinical development, a new scalable synthesis was required. Obatodax has been prepared using a three-step synthesis, starting from commercially available 4-methoxy-3-pyrrolin-2-one. The reaction sequence involves a haloformylation reaction followed by a Suzuki cross-coupling reaction with an indole-2-boronic add. The synthesis is completed by an acid-mediated condensation with 2,4-dimethyl-1H-pyrrole.

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More research is needed about 5-Methoxy-3,4-dihydro-2H-pyrrole

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PYRROLIDINOHYDROCHINAZOLINES

Disclosed are compounds of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, wherein the groups Ar1, Ar2, A, R1, R2, R3, E1, E2, X and n are as defined in the description and claims, which are effective modulators of chemokine activity.

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1-Pyrroline | C4H7N – PubChem

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One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, category: pyrrolines, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 73286-71-2, Name is N-Boc-2-pyrroline, molecular formula is C9H15NO2

Normal Alpha Olefin Synthesis Using Dehydroformylation or Dehydroxymethylation

The present invention discloses processes for producing normal alpha olefins, such as 1-hexene, 1-octene, 1-decene, and 1-dodecene in a multistep synthesis scheme from another normal alpha olefin. Also disclosed are reactions for converting aldehydes, primary alcohols, and terminal vicinal diols into normal alpha olefins.

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Simple exploration of 25021-08-3

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In heterogeneous catalysis, the catalyst is in a different phase from the reactants. Recommanded Product: 2-(2,5-Dioxo-2,5-dihydro-1H-pyrrol-1-yl)acetic acid, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 25021-08-3, name is 2-(2,5-Dioxo-2,5-dihydro-1H-pyrrol-1-yl)acetic acid. In an article£¬Which mentioned a new discovery about 25021-08-3

Transfer of stereochemical information in a minimal self-replicating system

The rational design, synthesis, and characterization of a minimal self-replicating system based on a 1,3-dipolar cycloaddition between a nitrone and a maleimide is presented. The importance of molecular recognition in this system is demonstrated using a competitive inhibitor. Doping experiments demonstrate that only one of the two diastereoisomeric products of the cycloaddition reaction is capable of acting as an efficient template for its own formation, accelerating the reaction between the nitrone and maleimide and controlling the stereochemical outcome of the reaction.

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1081-17-0, Name is 1-(4-Methoxyphenyl)-1H-pyrrole-2,5-dione, belongs to pyrrolines compound, is a common compound. Safety of 1-(4-Methoxyphenyl)-1H-pyrrole-2,5-dioneIn an article, once mentioned the new application about 1081-17-0.

Identifying cancer-related molecular targets of Nandina domestica Thunb. by network pharmacology-based analysis in combination with chemical profiling and molecular docking studies

Ethnopharmacological relevance: The fruits of Nandina domestica Thunb. have served as folk medicines in Chinese and Japanese tradition for treatment of several tumors including pharynx tumor and tooth abscess for many years, yet its exact mechanism of action is not yet known. Aim of the study: The study targets the identification of the main constituents of the fruits extracts and investigation of their mode of action in cancer therapy via pharmacology-based analysis and molecular docking. Materials and methods: The different extracts of N. domestica Thunb. were analyzed via UPLC?MS/MS for identification of their active constituents. STITCH, DAVID, KEGG and STRING database were utilized for construction of compound-target and compound-target-pathway networks using Cytoscape 3.2.1. Molecular docking analysis of the top hit compounds was performed against the identified top hit molecular targets in the constructed networks. In vitro-testing of Nandina domestica Thunb. against colorectal cancer cell lines was carried out and correlated to the chemical profile of the extract to identify important biomarkers. The ADME properties of the active compounds were also evaluated. Results: 22 compounds were identified by UPLC?MS/MS analysis and were forwarded to network pharmacology-based analysis. Results showed the enrichment of 5 compounds and 4 molecular targets in the network namely; AKT1, CASP3, MAPK1 and TP53. The pathway analysis of the identified targets revealed that 15 cancer-related pathways were enriched including colorectal cancer, endometrial cancer and small-cell lung cancer. In-vitro testing of the extracts against colo-rectal cancer cell lines revealed the fractions enriched in the identified hit compounds were indeed the most active as revealed from the HCA-heat-map. ADME results showed that all compounds were drug-like candidates showing acceptable values according to Lipinski’s rule. Conclusions: Network pharmacology analysis revealed that the compounds isoquercitrin, quercitrin, berberine, chlorogenic acid and caffeic acid showed strong synergistic interactions with the cancer-related targets and pathways. It could be concluded that N. domestica Thunb. constituents affect both apoptosis and Akt-signaling pathways during the stages of early and intermediate adenoma through interaction with the targets CASP3 and MAPK1 (ErC2) while during the stages of late adenoma and carcinoma, the compounds acts through the p53 and ErbB signaling pathways.

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Awesome Chemistry Experiments For 1-(4-Methoxyphenyl)-1H-pyrrole-2,5-dione

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New anti-Alzheimer drugs from biodiversity: The role of the natural acetylcholinesterase inhibitors

Alzheimer’s disease (AD) is a progressive neurodegenerative pathology with severe economic and social impact. There is currently no cure, although cholinesterase inhibitors provide effective temporary relief of symptoms in some patients. Nowadays, drug research and development are based on the cholinergic hypothesis that supports the cognition improvement by regulation of the synthesis and release of acetylcholine in the brain. There are only four commercial medicines approved for treatment of AD, and natural products have played an important alternative role in the research for new acetylcholinesterase inhibitors, as exemplified through the discovery of galantamine. This profile conducts us to give in this paper an overview relating the several classes of natural products with anti-cholinesterasic activity as potential templates to the design of new selective and powerful anti-Alzheimer drugs.

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Pyrroline – Wikipedia,
1-Pyrroline | C4H7N – PubChem

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Comparison of anticancer activity and hplc-dad determination of selected isoquinoline alkaloids from thalictrum foetidum, berberis sp. And chelidonium majus extracts

Background: Plants are an important origin of natural substances that The raw material for various pharmaceutical and therapeutic applications due to The presence of phytochemicals, such as alkaloids. Alkaloids, which are found in different plant species, possess numerous biological activities. Some alkaloids have strong cytotoxic effects on various cancer cells. The search for new drugs to treat various cancers is one of The most important challenges of modern scientific research. Objective: This study aimed to investigate of cytotoxic activity of extracts that were obtained from Chelidonium Majus; Berberis sp.; Thalictrum foetidum containing various alkaloids on selected cancer cell lines. The aim was also The quantification of selected alkaloids in The investigated extracts by HPLC. Methods: The analysis of alkaloids contents were performed while using HPLC in reversed phase (RP) mode using Polar RP column and mobile phase containing acetonitrile, water, and ionic liquid. The cytotoxic effect of The tested plant extracts and respective alkaloids’ standards were examined while using human pharyngeal squamous carcinoma cells (FaDu), human tongue squamous carcinoma cells (SCC-25), human breast adenocarcinoma cell line (MCF-7), and human triple-negative breast adenocarcinoma cell line (MDA-MB-231). Conclusion: All of The investigated plant extracts possess cytotoxic activity against cancer cell lines: FaDu, SCC-25, MCF-7, and MDA-MB-231. The highest cytotoxic activity against FaDu and MDA-MB-231 cells was observed for Chelidonium majus root extract, while the highest cytotoxic activity against SCC-25 and MCF-7 cells was estimated for The Thalictrum foetidum root extract. There obtained significant differences in The cytotoxic activity of extracts that were obtained from The roots and herbs of Chelidonium majus and Thalictrum foetidum. Based on these results, investigated plant extracts can be recommended for further investigations of anticancer activity.

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A protecting group free synthesis of (¡À)-neostenine via the [5 + 2] photocycloaddition of maleimides

(Chemical Equation Presented) A concise, linear synthesis of the Stemona alkaloid (¡À)-neostenine is reported. Key features include an organocopper-mediated bislactone C2-desymmetrization for the stereoselective construction of the cyclohexane-lactone C,D-rings. The assembly of the fused pyrrolo[1,2-a]azepine core was achieved by application of a [5 + 2] maleimide photocycloaddition. A custom FEP flow reactor was used to successfully overcome the scale limitations imposed by a classical immersion well batch reactor. The synthesis was completed in 14 steps from furan, in 9.5% overall yield, without the use of any protecting groups.

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Lactim ethers in the synthesis of 1,2-polymethylene-4-quinazolones

Condensation of lactim ethers with amides of o-halogeno-substituted aromatic acids was investigated. Derivatives of 5,7,8,9,10,11-hexahydroazepino[1,2-a]quinazolin-5-one and 1,2,3,4-tetrahydropyrrolo-[1,2-a]quinazolin-5-one were obtained.

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