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Pin1 (Protein interacting with NIMA1) is a cis?trans isomerase and promotes the amide bond rotation of phosphoSer/Thr-Pro motifs in its substrates. Inhibition of Pin1 might be a novel strategy for developing anticancer agents. Herein, a series of pyrimidine derivatives were synthesized and their Pin1 inhibitory activities were evaluated. Among them, four compounds (2a, 2f, 2h and 2l) displayed potent inhibitory activities against Pin1 with IC50 values lower than 3 muM. This series of pyrimidine-based inhibitors presented time-dependent inhibition against Pin1. The structure?activity relationships on the 2-, 4- and 5-positions of the pyrimidine ring were analyzed in details, which would facilitate further exploration of new Pin1 inhibitors.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H16944N – PubChem

 

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The invention provides compounds of formula (I) wherein m, R1, n, R2, q, X, Y, R3, R4, R5, R6, R7and R8 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H16912N – PubChem

 

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Dendrimers are hyperbranched macromolecules having a perfectly defined and multifunctionalized structure, constituted of branches emanating radially from a central core. The structure of dendrimers is particularly modular, and can incorporate in different parts coordination complexes. In this review, we will present the interplay between dendrimers and coordination chemistry in three main fields: catalysis, materials, and biology. Most of the examples will be taken from the work done with phosphorus-containing dendrimers, but the pioneering work carried out with other dendrimers will be also presented. One of the major improvements that metallodendrimers have afforded concerning catalysis is their easy recovery and reuse, bridging the gap between homogeneous and heterogeneous catalysis. Another major improvement concerns the ?dendritic effect? which can afford impressive outcomes concerning the increase of yield and of enantioselectivity, together with a decrease of the leaching of metals, and consequently of waste. Dendrimers can be used also for the synthesis and stabilization of metallic nanoparticles, for the modification of metallic surfaces at the nanometric scale, and for the synthesis of mesoscopically ordered hybrid materials. Finally metallodendrimers have high potency against cancerous cell lines, and they appear to operate via a different mechanism of action compared with native metallodrugs, opening new avenues for the search of improved anti-cancer agents.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H16982N – PubChem

 

Extracurricular laboratory:new discovery of 3-(Piperidin-4-ylmethyl)-1H-indole

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Protein tyrosine phosphatase (PTPase) 1B (PTP1B) has been implicated as a key negative regulator of both insulin and leptin signaling cascades. We identified several salicylic acid-based ligands for the second phosphotyrosine binding site of PTP1B using a NMR-based screening. Structure-based linking with a catalytic site-directed oxalylarylaminobenzoic acid-based pharmacophore led to the identification of a novel series of potent PTP1B inhibitors exhibiting 6-fold selectivity over the highly homologous T-cell PTPase (TCPTP) and high selectivity over other phosphatases.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H16938N – PubChem

 

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A number of unprecedented homo heteracalix[2]arene[2]triazines were synthesized by means of a fragment coupling approach. Two directional nucleophilic substitution reactions of N-Boc-protected 1,3-dihydrazobenzene with cyanuric acid chloride and 2-butoxy-4,6-dichloro-1,3,5-triazine led to hydrazo-linked trimers, which underwent an efficient macrocyclic condensation reaction with functionalized resorcinol derivatives to afford (NHNBoc)2,O2-calix[2]arene[2]triazine macrocycles, which contain a functional group either on the upper rim or the lower rim. The use of 1,3-phenylenediamines instead of resorcinol in the reaction produced (NR)2,(NHNBoc)2-calix[2]arene[2]triazines. Postmacrocyclization modifications such as a nucleophilic substitution reaction of chloro on triazine by amines and the removal of Boc from hydrazo moieties produced homo calix[2]arene[2]triazine derivatives. In the solid state, (NHNR)2,O2-bridged calix[2]arene[2]triazines with and without a substituent on the upper rim position and (NMe)2,(NHNBoc)2-calix[2]arene[2]triazine adopted a typical partial cone conformation while the heavily twisted 1,3-alternate conformational structures were observed for both (NHNBoc)2,O2-calix[2]arene[2]triazines bearing a functional group on the lower rim position and (NH)2,(NHNBoc)2-calix[2]arene[2]triazine. In solution, all synthesized homo heteracalix[2]arene[2]triazines existed as the mixture of different macrocyclic conformers, which underwent slow interconversions at room temperature relative to the NMR time scale.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H17025N – PubChem

 

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A series of phenylenebis(oxy)bis[2,2-dimethylpentanoic acid]s have been synthesized and evaluated as potential hypolipidemic agents. Compound 18 (CI-924) was found to be the most potent compound in this series. In rats, compound 18 is not only reduced low-density lipoprotein cholesterol but also increased high-density lipoprotein (HDL cholesterol. Comparative studies in rats indicated 18 produced an equal elevation of HDL cholesterol at one-third of the dose required of gemfibrozil. Structure-activity relationships are discussed.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H17015N – PubChem

 

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The present invention provides compounds of formula (I), wherein k, Ar, R2, R3, R4, R5, R4′, R5′, R6, R7, A, D, m and E are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H16896N – PubChem

 

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The Balz?Schiemann reaction endures as a method for the preparation of (hetero)aryl fluorides yet is eschewed due to the need for harsh conditions or high temperatures along with the need to isolate potentially explosive diazonium salts. In a departure from these conditions, we show that various organotrifluoroborates (RBF3?s) may serve as fluoride ion sources for solution-phase fluoro-dediazoniation in organic solvents under mild conditions. This methodology was successfully extended to a one-pot process obviating aryl diazonium salt isolation. Sterically hindered (hetero)anilines are fluorinated under unprecedentedly mild conditions in good-to-excellent yields. Taken together, this work expands the repertoire of RBF3?s to act as fluorine ion sources in an update to the classic Balz?Schiemann reaction.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H16926N – PubChem

 

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Because enzymes can increase reaction rates by enormous factors and tend to be very specific, Computed Properties of C14H18N2, typically producing only a single product in quantitative yield, they are the focus of active research.you can also check out more blogs about 3515-49-9

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A highly efficient and environmentally benign protocol for the synthesis of 8-amino-6-aryl-1,2-dihydro-2-oxo-6H-pyrano[2,3-e]benzoxazole-7-carbonitrile derivatives by one-pot threecomponent coupling reacting of aromatic aldehydes, malononitrile and 4-hydroxy-2(3H)-benzoxazolone under reflux condition has been developed in aqueous media using Na2O-Al2O3-P2O5 glass-ceramic system.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H17031N – PubChem

 

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Chemistry is traditionally divided into organic and inorganic chemistry. SDS of cas: 3515-49-9. The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent,Which mentioned a new discovery about 3515-49-9

The experimentally determined apparent rate constant (kapp) shows that the [BmIm]2[PdCl4] and [BmIm]2[NiCl4] act as effective catalysts for the reduction of nitroarenes to aminoarenes in the presence of NaBH4. The TEM, XPS, XRD and dynamic light scattering studies show that there is in situ formation of Pd and Ni metal Nanoparticles (NPs) from the reduction of [BmIm]2[PdCl4] and [BmIm]2[NiCl4], respectively which are responsible for the enhancement in the catalytic activity. Thus, in the presence of the ionic liquid stabilized metal NPs show higher catalytic activity in comparison to the NPs stabilized with other capping agents as reported. The order of kapp as 1) PNP > 2-BrPNP > 2-APNP and 2) PNP > ONP > 2-NR for reduction of nitroarenes using [BmIm]2[PdCl4] and [BmIm]2[NiCl4] and its correlation explained on the basis of electronic structure and hydrogen bonding ability of nitroarenes. The thermodynamic parameters such as Ea, ?H#, ?S# and ?G# are in agreement with the surface catalyzed reduction reaction of PNP in the presence of NPs as catalyst. The kapp values illustrated the reduction reaction follow the Langmuir-Hinshelwood (L-H) mechanism.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H16919N – PubChem