Awesome Chemistry Experiments For 73874-95-0

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Isocorydine (ICD), an aporphine alkaloid, is widely distributed in nature. Its ability to target side population (SP) cells found in human hepatocellular carcinoma (HCC) makes it and its derivative 8-amino-isocorydine (NICD) promising chemotherapeutic agents for the treatment of HCC. To improve the anticancer activity of isocorydine derivatives, twenty derivatives of NICD were designed and synthesized through chemical structure modifications of the aromatic amino group at C-8. The anti-proliferative activities of all synthesized compounds against human hepatocellular (HepG2), cervical (HeLa), and gastric (MGC-803) cancer cell lines were evaluated using an MTT assay. The results showed that all the synthetic compounds had some tumor cell growth inhibitory activity. The compound COM33 (24) was the most active with IC50 values under 10 muM (IC50 for HepG2 = 7.51 muM; IC50 for HeLa = 6.32 muM). FICD (12) and COM33 (24) were selected for further investigation of their in vitro and in vivo activities due to their relatively good antiproliferative properties. These two compounds significantly downregulated the expression of four key proteins (C-Myc, beta-Catenin, CylinD1, and Ki67) in HepG2 cells. The tumor inhibition rate of COM33 (24) in vivo was 73.8% after a dose 100 mg/kg via intraperitoneal injection and the combined inhibition rate of COM33 (24) (50 mg/kg) with sorafenib (50 mg/kg) was 66.5%. The results indicated that these isocorydine derivatives could potentially be used as targeted chemotherapy agents or could be further developed in combination with conventional chemotherapy drugs to target cancer stem cells (CSCs) and epithelial-to-mesenchymal transition (EMT), the main therapeutic targets in HCC.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H14171N – PubChem

 

A new application about tert-Butyl 2-oxa-7-azaspiro[3.5]nonane-7-carboxylate

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A detailed synthesis of novel spirocyclic oxetane analogs is described for the first time.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H18034N – PubChem

 

Extracurricular laboratory:new discovery of 203662-51-5

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Application of 203662-51-5, 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. 203662-51-5, Name is 4-Allyl-1-Boc-4-hydroxypiperidine, molecular formula is C13H23NO3. In a Article,once mentioned of 203662-51-5

A novel, selective, and efficacious GPR4 antagonist 13 was developed starting from lead compound 1a. While compound 1a showed promising efficacy in several disease models, its binding to a H3 receptor as well as a hERG channel prevented it from further development. Therefore, a new round of optimization addressing the key liabilities was performed and led to discovery of compound 13 with an improved profile. Compound 13 showed significant efficacy in the rat antigen induced arthritis as well as in the hyperalgesia and angiogenesis model at a well-tolerated dose of 30 mg/kg.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H20039N – PubChem

 

Simple exploration of 1-tert-Butyl 3-ethyl 4-aminopiperidine-1,3-dicarboxylate

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Disclosed herein are dihydroceramide desaturase 1 (Des1) inhibitor compounds and compositions, which are useful in the treatment of diseases, such as metabolic, cardiovascular, fibrotic, autoimmune/chronic inflammatory diseases, cystic fibrosis, various cancers, neurodegenerative diseases, lipid storage disorders, and ischemia/reperfusion injury, where inhibition of Des1 is expected to be therapeutic to a patient. Methods of inhibition of Des1 activity in a human or animal subject are also provided.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H22168N – PubChem

 

Brief introduction of (R)-tert-Butyl piperidin-3-ylcarbamate

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The invention relates to a synthesis method of chiral aminopiperidine and derivatives thereof. 3 . The invention is carried out by R (or S) – piperidine -3 – ethyl ester – L (or D) – L (or D)-tartrate after benzyl protection followed by azide and Curtitius rearrangement to R or S -benzyl -3 -aminopiperidine. R or S – benzyl -3 – aminopiperidine undergoes debenzylation to give R or S -amino piperidine, R or S – benzyl -3 – aminopiperidine through 3 -t-butoxycarbonyl protection, for example. Of R or S – (3 – t-butoxycarbonyl amino) piperidine, R or S – (3 – t-butoxycarbonyl amino) piperidine under acidic conditions can give R or S – 3-aminopiperidine, corresponding salts. The synthesis method provides a low-cost, easily-industrialized chiral 3 -aminopiperidine with high optical purity and a method. (by machine translation)

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H13394N – PubChem

 

The Absolute Best Science Experiment for 137076-22-3

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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, 137076-22-3, molcular formula is C11H19NO3, introducing its new discovery. category: piperidines

Naphthyridine compounds and their use as inhibitors of HPK1 are described. The compounds are useful in treating HPK1-dependent disorders and enhancing an immune response. Also described are methods of inhibiting HPK1, methods of treating HPK1-dependent disorders, methods for enhancing an immune response, and methods for preparing the naphthyridine compounds.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H16328N – PubChem

 

Discovery of 287192-97-6

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Disclosed are thiazolyl-dihydro-quinazolines of general formula (I) wherein the groups R1 to R4 have the meanings given in the claims and specification, the isomers thereof, and processes for preparing these compounds and their use as pharmaceutical compositions.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H15661N – PubChem

 

The important role of 8-Boc-2,8-Diazaspiro[4.5]decane

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Pancreatic beta-cell membranes and presynaptic areas of neurons contain analogous protein complexes that control the secretion of bioactive molecules. These complexes include the neuroligins (NLs) and their binding partners, the neurexins (NXs). It has been recently reported that both insulin secretion and the proliferation rates of beta-cells increase when cells are co-cultured with full-length NL-2 clusters. The pharmacological use of full-length protein is always problematic due to its unfavorable pharmacokinetic properties. Thus, NL-2-derived short peptide was conjugated to the surface of polyamidoamine-based (PAMAM) dendrimers. This nanoscale composite improved beta-cell functions in terms of the rate of proliferation, glucose-stimulated insulin secretion (GSIS), and functional maturation. This functionalized dendrimer also protected beta-cells under cellular stress conditions. In addition, various novel peptidomimetic scaffolds of NL-2-derived peptide were designed, synthesized, and conjugated to the surface of PAMAM in order to increase the biostability of the conjugates. However, after being covered by peptidomimetics, PAMAM dendrimers were inactive. Thus, the original peptide-based PAMAM dendrimer is a leading compound for continued research that might provide a unique starting point for designing an innovative class of antidiabetic therapeutics that possess a unique mode of action.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H19597N – PubChem

 

Archives for Chemistry Experiments of 91419-52-2

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Chemistry is traditionally divided into organic and inorganic chemistry. name: 1-Boc-4-Cyanopiperidine. The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent,Which mentioned a new discovery about 91419-52-2

The present invention refers to novel imidazotriazinones or already trillion which is bloom the rice field derivatives, these tautomeric, their stereoisomers and mixtures, or their pharmaceutically acceptable salts; including the height which burns sacrifice effect because of having immunosuppressive effect and associated for preventing or treating disease is directed to pharmaceutical composition. (by machine translation)

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H15750N – PubChem

 

Can You Really Do Chemisty Experiments About 5-(Piperidin-1-yl)pentanoic acid hydrochloride

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A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, HPLC of Formula: C10H20ClNO2, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 49637-20-9, Name is 5-(Piperidin-1-yl)pentanoic acid hydrochloride, molecular formula is C10H20ClNO2. In a Patent, authors is ,once mentioned of 49637-20-9

Novel heterocyclic esters of benzopyranopyridines represented by the formula STR1 wherein R1 is hydrogen, lower alkyl, lower alkanoyl, cycloalkyl-lower alkyl, cycloalkyl-lower alkanoyl, lower alkenyl, lower alkynyl, halo-loweralkenyl, phenyl-lower alkyl, phenyl-lower alkenyl or phenyl-lower alkynyl; R2 is lower alkyl; R3 is an alkyl having one to twenty carbon atoms or a cycloalkyl-lower alkyl, Y is a straight or branched chain alkylene having one to eight carbon atoms, and R4 is a group of the formula STR2 a is an integer from 1 to 4, b is an integer from 1 to 4 and X is CH2, O, S or N–R5 with R5 being hydrogen or lower alkyl, with the limitation that when X is O, S or N–R5, a and b each must be 2 and R6 is hydrogen or a lower alkyl group bonded to a carbon in the ring; and the acid addition salts thereof.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H17915N – PubChem