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The present study assessed the biological potential of fourteen 1,3-thiazolidin-4-ones evaluating the antiglioma effect through decreasing of cell viability of glioblastoma multiform cells. The new compounds were efficient synthesized through multicomponent or multicomponent one-pot procedures in moderate to good yields (22?86%) from two arenealdehydes (4-(methylthio)benzaldehyde and 4-(methylsulfonyl)benzaldehyde), seven amines (aromatic and aliphatic) and mercaptoacetic acid. The compounds were identified and characterized by GC/MS and NMR, five of them by HRMS. Six thiazolidinones showed significant effect of decreasing cell viability compared to standard drug TMZ at 100 muM in 72 h in C6 cell line by MTT assay. The compounds 5b, 5e, 5g and 6e showed the best results in the screening at 100 muM and were analyzed at different concentrations (5, 25, 50, 100 and 250 muM). Compounds 5b and 5e showed statistical difference at 5 muM, 6e at 25 muM and 5g at 50 muM in 72 h of treatment. The cytotoxicity study in primary astrocytes cells was evaluated and none of fourteen compounds showed toxicity at 100 muM, eight of them were not cytotoxic at 250 muM, both in 72 h. In addition, the propidium iodide assay demonstrated that the compounds might induce cell death by necrosis. In conclusion, this work reports at least four compounds (5b, 5e, 5g and 6e) with potential anti-tumor effect against glioblastoma multiform cell presenting activity at low concentrations and safe profile of cytotoxicity.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H4174N – PubChem

 

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Two isostructural mononuclear cobalt(III) complexes, [Co(C 15H21N2O)(C8H7O 2)(N3)] (1) and [Co(C15H21N 2O) (C8H7O2)(NCS)] (2), were synthesized and characterized by elemental analysis, IR spectra, and X-ray single crystal structure determination. X-ray structural analysis indicates that both complexes crystallizing in the monoclinic space group P21/c, with a = 13.190(2)A, b = 12.842(2)A, c = 18.428(2)A, beta = 134.040(2), V = 2243.9(5)A3, Z = 4 for 1, and a = 8.1284(8)A, b = 15.6112(15)A, c = 18.9260(17)A, beta = 106.060(3), V = 2307.9(4)A3, Z = 4 for 2. The Co atom in each complex is coordinated by one Schiff base ligand, one 2-acetylphenolate ligand, and one pseudohalide ligand (N3 for 1 and NCS for 2), forming an octahedral geometry. Copyright Taylor & Francis Group, LLC.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H4088N – PubChem

 

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Potent, specific, non-peptide small-molecule inhibitors of the MDM2-p53 interaction were successfully designed. The most potent inhibitor (MI-63) has a Ki value of 3 nM binding to MDM2 and greater than 10 000-fold selectivity over Bcl-2/Bcl-xL proteins. MI-63 is highly effective in activation of p53 function and in inhibition of cell growth in cancer cells with wild-type p53 status. MI-63 has excellent specificity over cancer cells with deleted p53 and shows a minimal toxicity to normal cells.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H4415N – PubChem

 

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The present invention relates to the novel pyrazolodiazepine compounds which potently inhibit the activity of transglutaminase in a dose dependent manner. Accordingly, it has been confirmed that the inventive compounds show potent inhibiting effect on the hyper-activated transglutaminase when the transglutaminase is over-expressed. Therefore the compounds can be useful in treating or preventing the disease caused by increased activation of transglutaminase.

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Piperidine – Wikipedia,
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A mild and rapid method for the iodination of arenes that utilizes silver(I) triflimide as a catalyst for activation of N-iodosuccinimide has been developed. The transformation was found to be general for a wide range of anisole, aniline, acetanilide, and phenol derivatives and allowed the late-stage iodination of biologically active compounds such as PIMBA, a SPECT imaging agent of breast cancer, and (a?)-IBZM, a dopamine D2 receptor antagonist. The method was also modified for the radioiodination of arenes using a one-pot procedure involving the in situ generation of [125I]-N-iodosuccinimide followed by the silver(I)-catalyzed iodination.

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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, 27578-60-5, name is N-(2-Aminoethyl)piperidine, introducing its new discovery. Computed Properties of C7H16N2

Minaprine [3[(beta-morpholinoethyl)amino]4-methyl-6-phenylpyridazine dihydrochloride] is active in most animal models of depression and exhibits in vivo a dual dopaminomimetic and serotoninomimetic activity profile. In an attempt to dissociate these two effects and to characterize the responsible structural requirements, a series of 47 diversely substituted analogues of minaprine were synthesized and tested for their potential antidepressant, serotonergic, and dopaminergic activities. The structure-activity relationships show that dopaminergic and serotonergic activities can be dissociated. Serotonergic activity appears to be correlated mainly with the substituent in the 4-position of the pyridazine ring whereas the dopaminergic activity appears to be dependent on the presence, or in the formation, of a para-hydroxylated aryl ring in the 6-position of the pyridazine ring.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H4487N – PubChem

 

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A recent approach in anticancer chemotherapy envisages telomerase as a potentially useful target. An attractive strategy deals with the development of compounds able to stabilize telomeric DNA in the G-quadruplex folded structure and, among them, a prominent position is found in the perylenes. With the aim to further investigate the role of drug structure, in view of possible pharmaceutical applications, we synthesized a series of compounds related to PIPER, a well-known perylene-based telomerase inhibitor. We modified the number of condensed aromatic rings and introduced different side chains to modulate drug protonation state and extent of self-aggregation. Effective telomerase inhibition was induced by heptacyclic analogues only, some showing a remarkably wide selectivity index with reference to inhibition of Taq polymerase. G-quadruplex stabilization was monitored by circular dichroism and melting experiments. Cell cytotoxicity measurements indicated a poor short-term cell killing ability for the best G-quartet binders. Besides the presence of a planar seven-condensed ring system, the introduction of a cyclic amine in the side chains critically affects the selectivity window.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H4786N – PubChem

 

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Three Ni(II) complexes of cresol-based Schiffbase ligands, namely [Ni 2(L1)(NCS)3(H2O)2], (1) [Ni2(L2)- (CH3COO)(NCS)2(H 2O)] (2) and [Ni2(L3)(NCS)3] (3), (where L1 = 2,6-bis(N-ethylpyrrolidineiminomethyl)-4-methylphenolato, L2 = 2,6-bis(N-ethylpiperidineiminomethyl)-4-methylphenolato and L3 = 2,6-bis{N-ethyl-N-(3-hydroxypropyl iminomethyl)}-4- methylphenolato), have been synthesized and structurally characterized by X-ray single-crystal diffraction in addition to routine physicochemical techniques. Density functional theory calculations have been performed to understand the nature of the electronic spectra of the complexes. Complexes 1-3 when reacted with 4-nitrophenyl phosphate in 50:50 acetonitrile-water medium promote the cleavage of the O-P bond to form p-nitrophenol and smoothly convert 3,5-ditert- butylcatechol (3,5-DTBC) to 3,5-di-tert-butylquinone (3,5-DTBQ) either in MeOH or in MeCN medium. Phosphatase- and catecholase-like activities were monitored by UV-vis spectrophotometry and the Michaelis-Menten equation was applied to rationalize all the kinetic parameters. Upon treatment with urea, complexes 1 and 2 give rise to [Ni2(L1)(NCS)2(NCO)(H 2O)2] (1′) and [Ni2(L2)- (CH 3COO)(NCO)(NCS)(H2O)] (2′) derivatives, respectively, whereas 3 remains unaltered under same reaction conditions. Springer Science+Business Media B.V. 2011.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H4107N – PubChem

 

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The present invention relates to compounds of the formula and pharmaceutically acceptable salts and solvates thereof, and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such compounds as adenosine A2a receptor agonists.

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Piperidine | C5H4197N – PubChem

 

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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, 27578-60-5, name is N-(2-Aminoethyl)piperidine, introducing its new discovery. Quality Control of: N-(2-Aminoethyl)piperidine

Overexpression of P-glycoprotein (Pgp) is associated with multidrug resistance (MDR) of tumor cells to a number of chemotherapeutic drugs. Pgp inhibitors have been shown to effectively reverse Pgp-mediated MDR. We prepared a series of phenoxy-N-phenylacetamide derivatives and tested for their ability to inhibit Pgp as potential MDR reversing agents, using a Pgp over-expressing MCF-7/ADR cell line. Some of the synthesized compounds exhibited moderate to potent reversal activity. Of note, compound 4o showed a 3.0-fold increased inhibition compared with verapamil, a well-known Pgp inhibitor. In addition, co-treatment of the representative compound 4o and a substrate anticancer agent doxorubicin resulted in a remarkable increase in doxorubicin’s antitumor effect and inhibition of DNA synthesis in the MCF-7/ADR cell line. Taken together, these findings suggest that compound 4o could be a useful lead for development of a novel Pgp inhibitor for treatment of MDR.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H4431N – PubChem