Wyniki wyszukiwania dla: gly-his-lys derivatives
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Electrochemical simulation of enzymatic transformations studied for the selected antitumor acridine derivatives
PublikacjaThe elucidation of the metabolic pathways and the biotransformation mechanisms of potential drugs is a crucial point in drug development. It allows to know the activation routes of the new biologically active compounds, especially in respect to their possible toxicity. Generally, in vivo or in vitro experiments with liver microsomes or hepatocytes are performed. However, these testing schemes are tedious, time consuming and of...
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Synthesis of conjugates of amino-combretastatin with tuftsin derivatives as potential anticancer agents
PublikacjaOpisano syntezę nowych koniugatów 3'-N-(tuftsyno lub retro-tuftsyno)-amino-kombretastatyny jako potencjalnych związków przeciw-nowotworowych. Do syntezy amino-kombretastatyny (amino-CA-4) wykorzystano reakację Wittiga a koniugatów metodę DPPA. Mamy nadzieję, że połączenie pochodnych tuftsyny z amino-CA-4 wpłynie na polepszenie właściwości terapeutycznych CA-4.
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Fully scalable one-pot method for the production of phosphonic graphene derivatives
PublikacjaGraphene oxide was functionalized with simultaneous reduction to produce phosphonated reduced graphene oxide in a novel, fully scalable, one-pot method. The phosphonic derivative of graphene was obtained through the reaction of graphene oxide with phosphorus trichloride in water. The newly synthesized reduced graphene oxide derivative was fully characterized by using spectroscopic methods along with thermal analysis. The morphology...
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Solid-Contact Ion-Selective Electrodes with Highly SelectiveThioamide Derivatives of p-tert-Butylcalix[4]arene for theDetermination of Lead(II) in Environmental Samples
PublikacjaThioamide derivatives of p-tert-butylcalix[4]arene were used as ionophores in the development of solid-contact ion-selective electrodes based on conducting polymer poly(3,4-ethylenedioxythiophene)/polystyrene sulfonate (PEDOT/PSS) which was synthesized by electrodeposition on the glassy carbon electrodes. The typical ion-selective membranes with optionally two different plasticizers [bis(2-ethylhexyl)sebacate (DOS) and 2-nitrophenyl...
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Ultrasound assisted synthesis of 3-alkynyl substituted 2-chloroquinoxaline derivatives: Their in silico assessment as potential ligands for N-protein of SARS-CoV-2
PublikacjaIn view of recent global pandemic the 3-alkynyl substituted 2-chloroquinoxaline framework has been explored as a potential template for the design of molecules targeting COVID-19. Initial in silico studies of representative compounds to assess their binding affinities via docking into the N-terminal RNA-binding domain (NTD) of N-protein of SARS-CoV-2 prompted further study of these molecules. Thus building of a small library of...
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Enhanced Activity of P4503A4 and UGT1A10 Induced by Acridinone Derivatives C-1305 and C-1311 in MCF-7 and HCT116 Cancer Cells: Consequences for the Drugs’ Cytotoxicity, Metabolism and Cellular Response
PublikacjaActivity modulation of drug metabolism enzymes can change the biotransformation of chemotherapeutics and cellular responses induced by them. As a result, drug-drug interactions can be modified. Acridinone derivatives, represented here by C-1305 and C-1311, are potent anticancer drugs. Previous studies in non-cellular systems showed that they are mechanism-based inhibitors of cytochrome P4503A4 and undergo glucuronidation via UDP-glucuronosyltranspherase...
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Amberlyst-15 catalysed synthesis of novel indole derivatives under ultrasound irradiation: Their evaluation as serotonin 5‑HT2C receptor agonists
PublikacjaA series of indole based novel Schiff bases was designed as potential agonists of 5‑HT2C receptor that was supported by docking studies in silico. These compounds were synthesized via Amberlyst-15 catalysed condensation of an appropriate pyrazole based primary amine with the corresponding indole-3-aldehyde under ultrasound irradiation at ambient temperature. A number of target Schiff bases were obtained...
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Synthesis and biological activity of novel ester derivatives of N3-(4-metoxyfumaroyl)-(S)-2,3-diaminopropanoic acid containing amide and keto function as inhibitors of glucosamine-6-phosphate synthase
PublikacjaA short series of novel ester derivatives of N3-4-methoxyfumaroyl-(S)-2,3-diaminopropanoic acid (FMDP) containing amido or keto functions have been designed and synthesized. Their antifungal activity and inhibitory properties toward fungal glucosamine-6-phosphate synthase has also been evaluated. The obtained compounds 11-13 and 15-17 demonstrated good antifunga activity against Candida albicans. Compounds 11-13 displayed also...
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Design, synthesis and high antitumor potential of new unsymmetrical bisacridine derivatives towards human solid tumors, specifically pancreatic cancers and their unique ability to stabilize DNA G-quadruplexes
PublikacjaNew promising unsymmetrical bisacridine derivatives (UAs), have been developed. Three groupsincluding 36 compounds were synthesized by the condensation of 4-nitro or 4-methylacridinone, imi-dazoacridinone and triazoloacridinone derivatives with 1-nitroacridine compounds linked with anaminoalkyl chain. Cytotoxicity screening revealed the high potency of these compounds against severaltumor cell lines. Particularly, imidazoacridinone-1-nitroacridine...
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New potent steroid sulphatase inhibitors based on 6-(1-phenyl-1H-1,2,3-triazol-4-yl)naphthalen-2-yl sulphamate derivatives
PublikacjaIn the present work, we report a new class of potent steroid sulphatase (STS) inhibitors based on 6-(1-phenyl-1H-1,2,3-triazol-4-yl)naphthalen-2-yl sulphamate derivatives. Within the set of new STS inhibitors, 6-(1-(1,2,3-trifluorophenyl)-1H-1,2,3-triazol-4-yl)naphthalen-2-yl sulphamate 3L demonstrated the highest activity in the enzymatic assay inhibiting the STS activity to 7.98% at 0.5 µM concentration. Furthermore, to verify...
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Spectral and photophysical properties of some imidazo[1,2-a]purine derivatives related to acyclovir
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Simplifying biochemical tumorous bone remodeling models through variable order derivatives
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The lipophilicity estimation of 5-arylidene derivatives of (2-thio)hydantoin with antimycobacterial activity
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Imidazo-thiazine, -diazinone and -diazepinone derivatives. Synthesis, structure and benzodiazepine receptor binding
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Influence of cellulose fibers on physicochemical properties of biodegradable films based on polysaccharide derivatives
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Synthesis of conjugates of MDP and nor-MDP linked to tuftsin derivatives as potential immunomodulators
PublikacjaZsyntetyzowano nowe koniugaty muramylodipeptydu (MDP) i nor-muramylo-dipeptydu (nor-MDP) z pochodnymi tuftsyny zawierającymi wiązanie izopeptydowe na epsilon-aminowej grupie lizyny jako potencjalne immunomodulatory. Do syntezy wykorzystano metodę mieszanych bezwodników z chloromrówczanem izobutylu i N-metylomorfoliną w bezwodnym DMF. Końcowe produkty charakteryzowno za pomocą NMR, analizy elementarnej i analizy aminokwasowej na...
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Solid phase synthesis of conjugates of tuftsin analogues with 1-nitro-acridine derivatives
PublikacjaZsyntetyzowano na fazie stałej koniugaty 1-nitro-akrydyny z pochodnymi tuftsyny modyfikowanymi na grupie epsilon-aminowej lizyny prostymi aminokwasami, np. alaniną, valiną, beta-alaniną. Końcowe produkty były charakteryzowane za pomocą MS, NMR, analizy elementarnej i przekazane do badań ich aktywności przeciwnowotworowej.
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Complexation of amino acids derivatives in water by calix[4]arene phosphonic acids
PublikacjaSeries of the calix[4]arene phosphonic acids with various substituents at the lower rim was synthesized. Complexing properties of these receptors towards methyl esters of six amino acids strongly depended on the calix[4]arene conformation flexibility. The complex formation processes were monitored using 1H NMR spectroscopy (deuterated phosphate buffer at pD 7.3, 22 oC) and association constant values were evaluated. Inherently...
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Experimental and theoretical studies of the spectroscopic properties of simple symmetrically substituted diphenylacetylene derivatives
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Lipidation of Temporin-1CEb Derivatives as a Tool for Activity Improvement, Pros and Cons of the Approach
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New Chalcone Derivatives Containing 2,4-Dichlorobenzenesulfonamide Moiety with Anticancer and Antioxidant Properties
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The mechanism of overcoming multidrug resistance (MDR) of fungi by amphotericin B and its derivatives
PublikacjaPrzeprowadzono badania porównawcze w celu określenia aktywności i cytotoksyczności amfoterycyny B (AmB) i jej pochodnych wobec standardowego szczepu S. cerevisiae i jego transformantów zawierających geny C. albicans kodujące białka oporności wielolekowej (MDR) typu ABC i MFS. Pochodne AmB: amid 3-dimetyloaminopropylowy amfoterycyny B oraz ester metylowy N-metylo-N-D-fruktopiranozylo-amfoterycyny B wykazały efekt fungistatyczny...
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Comparative evaluation of new dihydropyrimidine and dihydropyridine derivatives perturbing mitotic spindle formation
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NK1 receptor binding of a few low molecular weight 3,5-bistrifluoromethylbenzene derivatives
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Synthesis of Fentanyl Triazole Derivatives and their Affinity for Mu-Opioid and Sigma-1 Receptors
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Comparison of the ability to induce apoptosis by acridine derivatives in solid tumor and leukemia cells
PublikacjaW pracy wykazano różną wrażliwość komórek nowotworowych do ulegania apoptozie pod wpływem pochodnych akrydyny.
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Efficient synthesis of N-benzyloxycarbonyl- and N-tert-butoxycarbonyl-(S)-isoserine and their derivatives
PublikacjaOpisano wydajną metodę syntezy N-benzyloksykarbonylo- i N-tert-butoksykarbo-nylo-(S)-izoseryny i jej pochodnych z kwasu L-jabłkowego poprzez odpowiednie oksazolidinony i hydrolizę tych połączeń za pomocą wodorotlenku benzylowo-trimetyloamoniowego.
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Synthesis of Usnic Acid Derivatives and Evaluation of Their Antiproliferative Activity against Cancer Cells
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Vitamin D derivatives enhance cytotoxic effects of H2O2 or cisplatin on human keratinocytes
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Synthesis and antimicrobial and nitric oxide synthase inhibitory activities of novel isothiourea derivatives
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The Oxolane Ring Opening of Some Muramic Acid Derivatives Under Acidic Conditions
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New Benzo[h]quinolin-10-ol Derivatives as Co-sensitizers for DSSCs
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9,9′-bifluorenylidene derivatives as novel hole-transporting materials for potential photovoltaic applications
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Effect of heterocycle donor in 2-cyanoacrylic acid conjugated derivatives for DSSC applications
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Synthesis and application of tetrazole di and triamide derivatives in ion-selective membrane electrodes
PublikacjaA number of tetrazole diamides and triamides have been synthesized and applied as ion carries in ion-selective membrane electrodes. Their selectivity and sensitivity were studied towards alkali, alkaline earth, transition and heavy metal cations. it was found that membranes doped with 3 and 2-nitrophenyl octyl ether exhibit an almost theoretial Nernstian response for NH+ over relatively wide concentration range. Elestrodes with...
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The Chemometric Evaluation of Antitumor Activity of Novel Benzensulfonamide Derivatives Based on their Physiochemical Properties
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QSAR Analysis of Selected Antimicrobial Structures Belonging to Nitro-derivatives of Heterocyclic Compounds
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Interaction of amphotericin B and its selected derivatives with membranes: molecular modeling studies
PublikacjaJest to praca przeglądowa obejmująca krytyczną analizę danych dotyczących oddziaływania amfoterycyny B (AmB) i jej wybranych, mniej toksycznych pochodnych, z błonami lipidowymi. Amfoterycyna B jest antybiotykiem przeciwgrzybowym ale ze względu na jej toksyczność trwają prace nad modyfikacjami chemicznymi tego związku. Celem molekularnym dla tego antybiotyku jest błona lipidowa i dlatego różnicowe powinowactwo AmB i jej pochodnych...
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Synthesis, spectroscopy and computational studies of some novelphosphorylated derivatives of quinoline-5,8-diones
PublikacjaThe neutral phosphorus nucleophiles such as R2P(=Y)M allowed the radical addition to 2-methyl-5,8-dioxo-5,8-dihydroquinoline-7-amine and N-(2-methyl-5,8-dioxo-5,8-dihydroquinolin-7-yl)acetamide giving exclusively O-phosphorylated products. All products were quantitatively prepared and characterized by microanalysis, and multinuclear NMR spectroscopy. Seven of them, have been characterized by single crystal X-ray diffraction method....
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Reactivity of Diimido Complexes of Molybdenum and Tungsten towards Lithium Derivatives of Diphosphanes and Triphosphanes
PublikacjaThe reaction of R2P–P(SiMe3)Li (R = tBu, iPr) with the diimido molybdenum complex [(ArN)2MoCl2·dme] (Ar = 2,6-iPr2C6H3; dme = 1,2-dimethoxyethane) yielded the side-oncoordinated phosphanylphosphinidene anionic complexes [(2,6-iPr2C6H3N)2Mo(Cl)(η2-P=PR2)]– (7Mo, 8Mo). The thermal decomposition of [(2,6-iPr2C6H3N)2M(Cl)(η2-P=PR2)]–[M = Mo (7Mo), W (8W)] to [(2,6-iPr2C6H3N)2M(Cl)(1,2-η-tBu2P=P–PtBu2)] [M = Mo (3Mo), W (3W)] was investigated...
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Investigation of poly(3,4-ethylenedioxythiophene) deposition method influence on properties of ion-selective electrodes based on bis(benzo-15-crown-5) derivatives
PublikacjaGlassy carbon electrodes modified by conductive polymers and membrane with derivatives of bis(benzo-15-crown-5) were tested as solid contact ion selective electrodes for K+ ions concentration determination. PEDOT with PSS, Cl- and ClO4- counter ions was electrochemically deposited onto glassy carbon substrates using four different electrochemical approaches (potentiostatic, galvanostatic, potentiodynamic and potentiostatic pulses)....
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Rengel Cane Sia Doctoral Candidate
OsobyI'm Rengel, born and raised in the Philippines. As an undergraduate I did kinetic modeling on Copper-catalyzed atom transfer radical addition (ATRA). Then I was inspired to do both theoretical and experimental studies, which led me to propose my master's thesis on Synthesis, Computational, Electrochemical, and Photoconductivity Studies on Naphthalene and its derivatives. This led to a master's degree in Chemistry in the Mindanao...
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Novel 2-alkythio-4-chloro-N-[imino(heteroaryl)methyl]benzenesulfonamide Derivatives: Synthesis, Molecular Structure, Anticancer Activity and Metabolic Stability
PublikacjaA series of novel 2-alkythio-4-chloro-N-[imino-(heteroaryl)methyl]benzenesulfonamide derivatives, 8–24, were synthesized in the reaction of the N-(benzenesulfonyl)cyanamide potassium salts 1–7 with the appropriate mercaptoheterocycles. All the synthesized compounds were evaluated for their anticancer activity in HeLa, HCT-116 and MCF-7 cell lines. The most promising compounds, 11–13, molecular hybrids containing benzenesulfonamide...
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Structure-based design and evaluation of novel N-phenyl-1H-indol-2-amine derivatives for fat mass and obesity-associated (FTO) protein inhibition
PublikacjaFat mass and obesity-associated (FTO) protein contributes to non-syndromic human obesity which refers to excessive fat accumulation in human body and results in health risk. FTO protein has become a promising target for anti-obesity medicines as there is an immense need for the rational design of potent inhibitors to treat obesity. In our study, a new scaffold N-phenyl-1H-indol-2-amine was selected as a base for FTO protein inhibitors...
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Relationship between electronic structure and geometry of silanethiols and their derivatives. Elucidation of copper group silanethiolates
PublikacjaWyznaczono strukturę elektronową wybranych silanotioli X3SiSH (dla X=H, C2H5, OCH3, F, Cl i Br) oraz powstalych z nich anionów. Geometrię i funkcje falowe wyznaczono przy użyciu teorii funcjonałów gęstości elektronowej DFT. Przeanalizowano wpływ efektów anomerycznych oraz wielkości calki nakładania sigma(Si-S) na obserwowane skrócenie wiązania Si-S przy deprotonowaniu silanotioli. Podano nowe wyjaśnienie wyjątkowo niskiej kwasowości...
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Synthesis of new conjugates of MDP and nor-MDP with retro-tuftsin derivatives as potential immunomodulators
PublikacjaZsyntetyzowano nowe analogi muramylodipeptydu (MDP) i nor-muramylo-dipeptydu (nor-MDP) z pochodnymi retro-tuftsyny jako potencjalne immunomodulatory. Przedstawiono także syntezę odpowiednich pochodnych retro-tuftsyny. Do syntezy wykorzystano metodę mieszanych bezwodników z chloromrówczanem izobutylu i N-metylomorfoliną w bezwodnym DMF.
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Conformational Preferences of Proline Derivatives Incorporated into Vasopressin Analogues: NMR and Molecular Modelling Studies
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An In Vitro Antimicrobial, Anticancer and Antioxidant Activity of N–[(2–Arylmethylthio)phenylsulfonyl]cinnamamide Derivatives
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Can Immobilized Artificial Membrane Chromatography Support the Characterization of Antimicrobial Peptide Origin Derivatives?
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Skin cancer, including related pathways and therapy and the role of luteolin derivatives as potential therapeutics
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