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For developing novel therapeutic agents with anticancer activities, two series of novel 2,4-diaminopyrimidine derivatives possessing triazolopiperazine or 1,4,8-triazaspiro[4.5]decan-3-one scaffolds were designed and synthesized. Preliminary investigations showed that some compounds exhibited moderate to excellent potency against four tested cancer cell lines as compared with palbociclib and momelotinib. In particular, the most promising compounds 9k and 13f showed the most potent antitumor activities with IC50 values of 2.14/1.98 muM, 3.59/2.78 muM, 5.52/4.27 muM, and 3.69/4.01 muM against A549, HCT-116, PC-3 and MCF-7 cell lines, respectively. Structure-activity relationship (SAR) studies were conducted based on the variation of the moiety of the aromatic ring and the terminal aniline on the pyrimidine core. Furthermore, the mechanism of their anticancer activity was clarified by further exploring the bioactivity. The results showed that compound 9k obviously inhibited the proliferation of A549 cell lines, induced a great decrease in the mitochondrial membrane potential leading to apoptosis of cancer cells, suppressed the migration of tumor cells and prolonged the A549 cell cycle distribution, representing blockage at the G2-M phase and accumulation at the S phase.

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Piperidine – Wikipedia,
Piperidine | C5H10592N – PubChem

 

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The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 2359-60-6 is helpful to your research. Computed Properties of C11H16N2

In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 2359-60-6, name is 4-Piperidinoaniline, introducing its new discovery. Computed Properties of C11H16N2

Highly potent and selective small molecule neuropeptide Y Y2 receptor antagonists are reported. The systematic SAR exploration of a hit molecule N-(4-ethoxyphenyl)-4-[hydroxy(diphenyl)methyl]piperidine-1-carbothioamide, identified from HTS, led to the discovery of highly potent NPY Y2 antagonists 16 (CYM 9484) and 54 (CYM 9552) with IC50 values of 19 nM and 12 nM respectively.

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Piperidine | C5H10588N – PubChem

 

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The present invention provides the para-substituted cyclic amine containing diamine monomer of the triphenylamine structure, preparation method and its application in the preparation of polyamide, which belongs to the technical field of preparation of organic compounds. Synthetic method is divided into four-step, cyclic amine compound with P-nitrobenzene under the action of the potassium carbonate, obtained through nucleophilic substitution reaction of cyclic amine structure containing single nitro compound; used as a catalyst after Pd/C, hydrazine hydrate as reducing agent containing cyclic amine structure of the obtained single-amino-containing compound; and then the single-amino compound cesium fluoride with P-nitrobenzene under the action of the, through nucleophilic substitution reaction of para-substituted cyclic amine containing dinitro monomer triphenylamine structure; finally Pd/C as the catalyst, the reducing agent is hydrazine hydrate containing para-substituted cyclic amine triphenylamine diamine monomer structure. The diamine monomer with a plurality of the second acid reaction can be made of polyamide with electrochromic properties. (by machine translation)

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Piperidine | C5H10552N – PubChem

 

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Dye-donor element for use according to thermal dye sublimation transfer, said dye-donor element comprising a support provided with a dye layer containing a dye dispersed in a polymeric binder, characterized in that said dye corresponds to the following formula (I) wherein, R¹, R² and R³ independently represent hydrogen, halogen, nitro, an alkyl group, a cycloalkyl group, an aryl group, an alkoxy group, an aryloxy group, a alkylthio group, a arylthio group, an acylamino group, a sulfamoyl group, a carbamoyl group, which groups may be substituted, or R² and R³ together can form a saturated or aromatic or heterocyclic ring fused-on the cyclohexadiene ring, which ring may be substituted; wherein, R4 represents hydrogen, an alkyl group, a cycloalkyl group, an aryl group, which groups may be substituted, SO2R¹0, COR¹0, POR¹0R¹¹;, R5 represents hydrogen, halogen, nitro, cyano, an alkyl group, an aryl group, an alkoxy group, an alkylthio group, which groups may be substituted;, R6 and R6’independently represent an alkyl group, a cycloalkyl group, an alkenyl group, an aralkyl group, an aryl group, an alkoxy group, an aryloxy group, an alkylthio group, an arylthio group, an amino group or a heterocyclic group, which groups may be substituted, or R6 and R6’together form a 5- or 6-membered ring, which ring may be substituted;, R7 represents an alkyl group, an aryl group, a cycloalkyl group, which groups may be substituted;, R8 and R9 independently represent hydrogen, an alkyl group,an aryl group, a cycloalkyl group, which groups may be substituted, or R8 and R9 together can form a heterocyclic ring, which ring may be substituted;, R¹0 and R¹¹ independently represent an alkyl group, a cycloalkyl group, an alkenyl group, an aralkyl group, an aryl group, an alkoxy group, an aryloxy group, an alkylthio group, an arylthio group, an amino group or a heterocyclic group, which groups may be substituted, or R¹0 and R¹¹ together form a 5- or 6-membered ring, which ring may be substituted;, K represents wherein:, R¹² and R¹³ (independently) represent hydrogen, an alkyl group, an aryl group, a heterocyclic group, which groups may be substituted, or R¹² and R¹³ together represent the necessary atoms to close a heterocyclic ring, which ring may be substituted, or R¹² and/or R¹³ together with R¹4 and/or R¹7 represent the necessary atoms to close a ring fused-on the benzene ring, which ring may be substituted;, R¹4, R¹5, R¹6 and R¹7 independently represent hydrogen, hydroxy, halogen, an alkyl group, a cycloalkyl group, an aryl group, an alkyloxy group, an aryloxy group, a carbamoyl group, a sulfamoyl group, which groups may be subsituted which groups may be substituted, NH-SO2R¹8, NH-COR¹8, O-SO2R¹8, O-COR¹8, or R¹4 and R¹5 together and/or R¹6 and R¹7 together represent the necessary atoms to close (a) ring(s) fused-on the benzene ring or R¹4 and/or R¹7 together with R¹² and/or R¹³ represent the necessary atoms to close a heterocyclic ring fused-on the benzene ring, which groups may be substituted;, R¹8 represents an alkyl group, a cycloalkyl group, an alkenyl group, an aralkyl group, an aryl group, an alkyloxy group, an aryloxy group, an alkylthio group, an arylthio group, an amino group, a heterocyclic group, which groups may be substituted.

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Piperidine – Wikipedia,
Piperidine | C5H10598N – PubChem

 

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The present invention relates to compounds of formula (I), which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, syndrome X, hyperinsulinemia, obesity, atherosclerosis, and various immunomodulatory diseases.

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Awesome Chemistry Experiments For 4-Piperidinoaniline

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Related Products of 2359-60-6, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.2359-60-6, Name is 4-Piperidinoaniline, molecular formula is C11H16N2. In a article,once mentioned of 2359-60-6

To develop novel therapeutic agents with anticancer activities, two series of novel 7-amino-[1,2,4]triazolo[4,3-f]pteridinone, and 7-aminotetrazolo[1,5-f]pteridinone derivatives were designed and synthesized. All compounds were tested for anti-proliferative activities against five cancer cell lines. The structure-activity relationships (SARs) studies were conducted through the variation in two regions, the moiety of A ring and the terminal aniline B on pteridinone core. 1-Methyl-1,2,4-triazole derivative L7 with 2,6-dimethylpiperazine showed the most potent antiproliferative activity against A549, PC-3, HCT116, MCF-7 and MDA-MB-231 cell lines with IC50 values of 0.16 muM, 0.30 muM, 0.51 muM, 0.30 muM, and 0.70 muM, respectively. Combined with the results of the molecular docking and enzymatic studies, the PLK1 was very likely to be one of the drug targets of compound L7. Furthermore, to clarify the anticancer mechanism of compound L7, further explorations in the bioactivity were conducted. The results showed that compound L7 obviously inhibited proliferation of A549 cell lines, induced a great decrease in mitochondrial membrane potential leading to apoptosis of cancer cells, suppressed the migration of tumor cells, and arrested G1 phase of A549 cells.

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Reference:
Piperidine – Wikipedia,
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Discovery of pteridin-7(8 H)-one-based irreversible inhibitors targeting the epidermal growth factor receptor (EGFR) kinase T790M/L858R mutant

The EGFR T790M variant is an important mutation, resulting in approximately 50% of the clinically acquired resistance to approved EGFR inhibitors. Starting with a previously reported pyrimidine-based EGFR inhibitor, a novel pteridin-7(8H)-one scaffold with a high 3D similarity was found and transformed into irreversible inhibitors of the EGFR T790M mutant. The most potent compounds, 3q and 3x, exhibited excellent enzyme inhibitory activities, with subnanomolar IC50 values for both the wild-type and T790M/L858R double mutant EGFRs, as well as potent cellular antiproliferative activities against both gefitinib-sensitive and -resistant cancer cell lines. The in vivo antitumor efficacy study demonstrated that compound 3x significantly inhibited tumor growth and induced tumor stasis in an EGFR-T790M/L858R-driven human nonsmall-cell lung cancer xenograft mouse model. This work demonstrated the utility of this sophisticated computational design strategy for fast 3D scaffold hopping with competitive bioactivities to meet an important clinical need.

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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, 2359-60-6, molcular formula is C11H16N2, introducing its new discovery. Recommanded Product: 2359-60-6

Design and structure-activity relationships of potent and selective inhibitors of undecaprenyl pyrophosphate synthase (UPPS): Tetramic, tetronic acids and dihydropyridin-2-ones

Based on a pharmacophore hypothesis substituted tetramic and tetronic acid 3-carboxamides as well as dihydropyridin-2-one-3-carboxamides were investigated as inhibitors of undecaprenyl pyrophosphate synthase (UPPS) for use as novel antimicrobial agents. Synthesis and structure-activity relationship patterns for this class of compounds are discussed. Selectivity data and antibacterial activities for selected compounds are provided.

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Antibacterial barbituric acid analogues inspired from natural 3-acyltetramic acids; Synthesis, tautomerism and structure and physicochemical property-antibacterial activity relationships

The synthesis, tautomerism and antibacterial activity of novel barbiturates is reported. In particular, 3-acyl and 3-carboxamidobarbiturates exhibited antibacterial activity, against susceptible and some resistant Gram-positive strains of particular interest is that these systems possess amenable molecular weight, rotatable bonds and number of proton-donors/acceptors for drug design as well as less lipophilic character, with physicochemical properties and ionic states that are similar to current antibiotic agents for oral and injectable use. Unfortunately, the reduction of plasma protein affinity by the barbituric core is not sufficient to achieve activity in vivo. Further optimization to reduce plasma protein affinity and/or elevate antibiotic potency is therefore required, but we believe that these systems offer unusual opportunities for antibiotic drug discovery.

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Piperidine | C5H10536N – PubChem

 

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Multicomponent reactions for facile access to coumarin-fused dihydroquinolines and quinolines: Synthesis and photophysical studies

A simple and straightforward method for facile access to coumarin-fused dihydroquinolines (4) has been developed using the microwave-assisted multicomponent reactions of 4-hydroxycoumarin, aldehydes and aromatic amines in water catalyzed by bismuth triflate. Under solvent-free and conventional heating conditions, the same combination provided the corresponding coumarin-fused quinolines (5). An alternative and rapid method for the conversion of (4) to (5) with very good yields was also developed using N-bromosuccinamide. Single-crystal X-ray crystallographic analysis of one of the products (4q) showed that the products are regioselective and that the reactions proceed via 1,2-addition followed by 6pi-electrocyclization instead of a Skraup-Doebner-von Miller type reaction. Substituted quinoline carboxylic acid derivatives (7) were synthesized selectively from (4) by ring opening of the coumarin moiety followed by aromatization using NaOH/DMSO under reflux conditions. Considering the presence of the polycyclic conjugated structure of the synthesized compounds 4 and 5 with the coumarin moiety, preliminary photophysical studies were carried out and promising quantum yields were observed along with a maximum quantum yield (of = 0.65) for 4j.

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