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We report the development of molecular hybrids in which a nitrate group serving as nitric oxide (NO) donor is covalently joined to sigma receptor ligands to give candidates for double-targeted cancer therapy. The compounds have been evaluated in radioligand binding assay at both sigma receptors and selected compounds tested for NO release. Compounds 9, 15, 18, 19, and 21 were subjected to MTT test. Compound 15 produced a significant reduction of MCF-7 and Caco-2 cellular viability with comparable IC50 as doxorubicin, being also not toxic for fibroblast HFF-1 cells. Compound 15 has shown a sigma1 receptor antagonist/sigma2 receptor agonist profile. Two derivatives of compound 15 lacking the nitrate group did not induce a reduction of MCF-7 cellular

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H12110N – PubChem

 

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The present invention relates to a novel method for synthesizing imidazole derivatives having 4-aryl, 5-pyrimidine heterocyclic rings using a novel cycloaddition reaction.

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Piperidine – Wikipedia,
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The title compounds, Methyl N-(4-methoxyphenylmethyl)- N0- cyanocarbamimidothioate, I, and Methyl N-[1-(phenylmethyl)-4-piperidinyl]-N0- cyanocarbamimidothioate, II, have been designed and synthesized for use as new potential organic molecular electronic materials. The crystal structure of I and II were determined with crystal data (I: Monoclinic, P21/c, a = 4.746(2) a , b = 5.737(3) a , c = 17.399(7) a , b = 91.667(7)8, Rall = 0.0703; II: Orthorhombic, Pna21, a = 18.209(8) a , b = 11.463(5) a , c = 7.539(3) a , b = 90.00 8, Rall = 0.0481). N-HN hydrogen bonds were responsible for the formation of onedimensional zigzag molecular chains of I, and trifurcated hydrogen-bonded molecular chains were indicated in structure of II. C-Hpi and C-HN hydrogen bonds were found in both structures. All these types of interaction together form an extended three-dimensional network and stabilize the title crystals. Springer Science+Business Media, LLC 2011.

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Piperidine – Wikipedia,
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More research is needed about 4-Amino-1-benzylpiperidine

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The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the histamine-3 receptor.

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A series of 1- and 2-naphthamides has been prepared and tested for in vitro binding to D2L, D4.2, and 5-HT2A receptors. Different compounds display selectivity for D4.2 and 5-HT2A receptors versus D2L receptors. N-(1-Arylalkyl-piperidin-4-yl) carboxamides have higher affinities than the corresponding N-(4-arylalkylamino-piperidin-1-yl) carboxamide analogues. A benzyl moiety in position 1 of the piperidine in the 2-naphthamide series (2) appears to be the best choice for a favorable interaction with D4.2 and 5-HT2A receptors. Increasing the linker length between the phenyl ring and the basic nitrogen led to a decreased affinity for these receptors. In the 1-naphthamide series, the most potent D4.2 ligand (7) possesses a phenylpropyl moiety while its affinity for 5-HT2A receptors is strongly reduced. All compounds with significant affinity for D4.2 and 5-HT2A receptors were antagonists.

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Final Thoughts on Chemistry for 50541-93-0

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 50541-93-0 is helpful to your research. Synthetic Route of 50541-93-0

Synthetic Route of 50541-93-0, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.50541-93-0, Name is 4-Amino-1-benzylpiperidine, molecular formula is C12H18N2. In a Article,once mentioned of 50541-93-0

A solid phase method for the synthesis of glutamic acid derivatives based on the chemoselective ring opening of N-Boc pyroglutamic-Wang resin by heteronucleophiles is described. It allows the preparation of a large number of amides and esters of glutamic acid in a simple procedure with moderate to good yields and excellent purity. (C) 2000 Elsevier Science Ltd.

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Piperidine – Wikipedia,
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Discovery of 50541-93-0

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The present invention relates to a process for preparing the compound 3-(4-piperidinyl)-2,3,4,5-tetrahydro-1,3-benzodiazepin-2(1-one of formula which is to be found as a structural element in CGRP-antagonists, which are particularly suitable for the oral treatment of migraine.

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Piperidine – Wikipedia,
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Previously, we have found that BRN-103, a nicotinamide derivative, inhibits vascular endothelial growth factor (VEGF)-mediated angiogenesis signaling in human endothelial cells. During our continuous efforts to identify more potent anti-angiogenic agents, we synthesized various nicotinamide derivatives and evaluated their anti-angiogenic effects. We found that 2-{1-[1-(6-chloro-5- fluoropyrimidin-4-yl)ethyl]piperidin-4-ylamino}-N-(3-chlorophenyl) pyridine-3-carboxamide (BRN-250) significantly inhibited human umbilical vascular endothelial cells (HUVECs) proliferation, migration, tube formation, and microvessel growth in a concentration range of 10-100 nM. Furthermore, BRN-250 inhibited the VEGF-induced phosphorylation and intracellular tyrosine kinase activity of VEGF receptor 2 (VEGFR2) and the activation of its downstream AKT pathway. Taken together, these findings suggest that BRN-250 be considered a potential lead compound for cancer therapy.

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Reference:
Piperidine – Wikipedia,
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A highly-efficient catalytic system for hydrodebenzylation reaction is described. The cleavage of O-benzyl and N-benzyl protecting groups was performed using an uncommonly low palladium loading (0.02?0.3 mol%; TON up to 5000) in a relatively short reaction time. The approach was used for a variety of substrates including pharmaceutically important precursors, and gram-scale deprotection reaction was shown. Transfer conditions together with easy-to-make Pd/C catalyst are the key features of this debenzylation scheme. (Figure presented.).

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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, 50541-93-0, molcular formula is C12H18N2, introducing its new discovery. Recommanded Product: 50541-93-0

Provided are certain cyclic urea compounds that are capable of inhibiting certain serine proteases, and especially the serine proteases matriptase, hepsin and hepatocyte growth factor activator (HGFA) involved in the maturation of hepatocyte growth factor (HGF) and macrophage stimulating protein (MSP), and novel precursors thereof. Compounds of the present disclosure can be used to treat a number of disorders caused by or associated with abnormal matriptase, hepsin and HGFA protease activity by inhibiting the proteolytic cleavage of pro-HGF to mature HGF and pro-MSP to mature MSP caused by these enzymes. Compounds of the present disclosure can be used to treat disorders including precancerous conditions and cancer including metastatic disease, prevention and reversion of cancer resistance, and the inhibition of cancer stem cells. The compounds of this invention are applicable to the treatment of cancers of many tissue types including solid and liquid tumors.

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