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Search results for: GLY-HIS-LYS DERIVATIVES
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Prediction of Overall In Vitro Microsomal Stability of Drug Candidates Based on Molecular Modeling and Support Vector Machines. Case Study of Novel Arylpiperazines Derivatives
PublicationOther than efficacy of interaction with the molecular target, metabolic stability is the primary factor responsible for the failure or success of a compound in the drug development pipeline. The ideal drug candidate should be stable enough to reach its therapeutic site of action. Despite many recent excellent achievements in the field of computational methods supporting drug metabolism studies, a well-recognized procedure to model...
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Stabilities of bisphenol A diglycidyl ether, bisphenol F diglycidyl ether, and their derivatives under controlled conditions analyzed using liquid chromatography coupled with tandem mass spectrometry
PublicationBisphenol A diglycidyl ether (BADGE), bisphenol F diglycydyl ether (BFDGE), and their related compounds are widely used as precursors in production of epoxy resins. The high reactivity of these compounds makes the development of analytical methodologies that ensure appropriate metrological accuracy crucial. Consequently, we aimed to determine whether and to what extent the composition of the solution and storage conditions affect...
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99mTc-Galacto-RGD2: A Novel 99mTc-Labeled Cyclic RGD Peptide Dimer Useful for Tumor Imaging
PublicationThis study sought to evaluate [99mTc(HYNIC-Galacto-RGD2)-(tricine)(TPPTS)] (99mTc-Galacto-RGD2: HYNIC = 6-hydrazinonicotinyl; Galacto-RGD2 = Glu[cyclo[Arg-Gly-Asp-D-Phe-Lys(SAA-PEG2-(1,2,3-triazole)-1-yl-4-ethylamide)]]2 (SAA = 7-amino-L-glycero-L-galacto-2,6-anhydro-7-eoxyheptanamide, and PEG2 = 3,6-dioxaoctanoic acid); and TPPTS = trisodium triphenylphosphine-3,3',3''-trisulfonate) as a new radiotracer for tumor imaging. Galacto-RGD2...
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Mass spectrometry based identification of geometric isomers during metabolic stability study of a new cytotoxic sulfonamide derivatives supported by quantitative structure-retention relationships
PublicationA set of 15 new sulphonamide derivatives, presenting antitumor activity have been subjected to a metabolic stability study. The results showed that besides products of biotransformation, some additional peaks occurred in chromatograms. Tandem mass spectrometry revealed the same mass and fragmentation pathway, suggesting that geometric isomerization occurred. Thus, to support this hypothesis, quantitative structure-retention relationships...
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Investigation of the Binding Properties of the Cosmetic Peptide Argireline and Its Derivatives Towards Copper(II) Ions
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Antitumor Activity of Novel Benzensulfonamide Derivatives in View of their Physiochemical Properties Searched by Principal Component Analysis
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Spectral Characteristic and Preliminary Anticancer Activity in vitro of Selected Rhodanine‐3‐carboxylic Acids Derivatives
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Fragmental Method KowWIN as the Powerful Tool for Prediction of Chromatographic Behavior of Novel Bioactive Urea Derivatives
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The oxydiacetate and iminodiacetate complexes of oxidovanadium(IV) as the new series of the catalysts for the oligomerization of beta-olefin derivatives
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Carboxymethylated starch and cellulose derivatives-based film as human skin equivalent for adhesive properties testing
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The new esters derivatives of betulin and betulinic acid in epidermoid squamous carcinoma treatment – In vitro studies
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Genetic and lifestyle variables associated with homocysteine concentrations and the distribution of folate derivatives in healthy premenopausal women
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Experimental and theoretical studies of spectroscopic properties of simple symmetrically substituted diphenylbuta-1,3-diyne derivatives
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Determining the true content of quercetin and its derivatives in plants employing SSDM and LC–MS analysis
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New chiral discotics with helical organization of the mesophase—liquid crystalline derivatives of dibenzotetraaza[14]annulene
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Molecular dynamics study on the influence of C-terminal sugar substitution on dynamics and conformation of vancomycin derivatives
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New D−π–D−π–A Systems Based on Phenothiazine Derivatives with Imidazole Structures for Photovoltaics
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Diosgenyl 2-amino-2-deoxy-β-D-galactopyranoside: synthesis, derivatives and antimicrobial activity
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Synthesis and SAR-study for novel arylpiperazine derivatives of 5-arylidenehydantoin with α1-adrenoceptor antagonistic properties
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Tricyclic xanthine derivatives containing a basic substituent: adenosine receptor affinity and drug-related properties
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Synthesis and biological activity of novel mycophenolic acid conjugates containing nitro-acridine/acridone derivatives
PublicationOpracowano warunki reakcji kwasu mykofenolowego z aminowymi pochodnymi akrydyn i akrydonów. Tak otrzymane koniugaty zostały scharakteryzowane, a następnie przebadane in vitro pod względem aktywności przeciwbiałaczkowej oraz immunosupresyjnej.
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Inactivation of glucosamine-6-phosphate synthase by N3-oxoacyl derivatives of L-2,3-diaminopropanoic acid
PublicationN3-oksoacylowe pochodne kwasu l-2,3-diaminopropanowego zawierające ugrupowanie epoksydowe lub układ sprzężonych wiązań podwójnych inaktywują syntaze glukozamino-6-fosforanu (GlcN-6-P) z S. cerevisiae. Wyniki badań kinetycznych inaktywacji enzymu wskazują na dwuetapowy przebieg tej reakcji, przy czym tworzenie kompleksu enzym:ligand poprzedza nieodwracalną modyfikację enzymu. Badane związki różniły się powinowactwem do centrum aktywnego...
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Chromogenic complexes and selective preconcentration of Fe(III) and Cu(II) by hydroxynaphthoyl-1,4,7,10-tetraazacyclododecane derivatives
PublicationSpektroskopowe oznaczanie zawartości jonów żelaza w różnych próbkach środowiskowych jest przedmiotem wieloletnich badań. Pomimo tego ciągle poszukuje się selektywnych odczynników zdolnych do tworzenia kompleksów z jonami żelaza(II) lub żelaza(III). 1,4,7,10-tetraazacyklododekan nie tworzy kompleksów z jonami żelaza, ale wprowadzając stosowne podstawniki można uzyskać właściwe ligandy. W reakcji acylowania otrzymano 1-(1-hydroksy-2-naftoilo)-1,4,7,10-tetraazacyklododekan...
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Derivatives of 1-nitroacridine induce apoptosis only in a limited number of human colon adenocarcinoma cells
PublicationPraca dotyczy indukcji apoptozy w komórkach ludzkich raków okrężnicy HT29 i HCT8 pod wpływem pochodnych 1-nitroakrydyny: C-857 i C-1748. Wykazano, że związki te w stężeniach biologicznie istotnych (EC90) indukują apoptozę tylko w części populacji komórek. Efekt ten uzależniony był od czasu inkubacji komórek ze związkiem, a nie zależał od stężenia związku.
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Comments on various extensions of the Riemann–Liouville fractional derivatives : About the Leibniz and chain rule properties
PublicationStarting from the Riemann–Liouville derivative, many authors have built their own notion of fractional derivative in order to avoid some classical difficulties like a non zero derivative for a constant function or a rather complicated analogue of the Leibniz relation. Discussing in full generality the existence of such operator over continuous functions, we derive some obstruction Lemma which can be used to prove the triviality...
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On the derivatives $\partial^{2}P_{\nu}(z)/\partial\nu^{2}$ and $\partial Q_{\nu}(z)/\partial\nu$ of the Legendre functions with respect to their degrees
PublicationWe provide closed-form expressions for the degree-derivatives $[\partial^{2}P_{\nu}(z)/\partial\nu^{2}]_{\nu=n}$ and $[\partial Q_{\nu}(z)/\partial\nu]_{\nu=n}$, with $z\in\mathbb{C}$ and $n\in\mathbb{N}_{0}$, where $P_{\nu}(z)$ and $Q_{\nu}(z)$ are the Legendre functions of the first and the second kind, respectively. For $[\partial^{2}P_{\nu}(z)/\partial\nu^{2}]_{\nu=n}$, we find that % \begin{displaymath} \frac{\partial^{2}P_{\nu}(z)}{\partial\nu^{2}}\bigg|_{\nu=n} =-2P_{n}(z)\Li_{2}\frac{1-z}{2}+B_{n}(z)\ln\frac{z+1}{2}+C_{n}(z), \end{displaymath} % where...
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New Unsymmetrical Bisacridine Derivatives Noncovalently Attached to Quaternary Quantum Dots Improve Cancer Therapy by Enhancing Cytotoxicity toward Cancer Cells and Protecting Normal Cells
PublicationThe use of nanoparticles for the controlled drug delivery to cells has emerged as a good alternative to traditional systemic delivery. Quantum dots (QDs) offer potentially invaluable societal benefits such as drug targeting and in vivo biomedical imaging. In contrast, QDs may also pose risks to human health and the environment under certain conditions. Here, we demonstrated that unique combination of nanocrystals core components...
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High yield synthesis and preliminary spectroscopic study of mono-N-alkylated cyclen derivatives of salicylic acid
PublicationW artykule przedstawiono reakcję bezpośredniego alkilowania cyklenu bromopochodnymi kwasu salicylowego. Otrzymane związki wykorzystano do badań spektroskopowych. Stwierdzono, że tworzą one wybiórczo kompleksy z jonami metali grupy II. Wyznaczono stałe tworzących się kompleksów.
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Exploring Alkyl Ester Salts of L-Amino Acid Derivatives of Ibuprofen: Physicochemical Characterization and Transdermal Potential
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Application of the PASSIL technique for the passive sampling of exemplary polar contaminants (pharmaceuticals and phenolic derivatives) from water
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Synthesis and SAR Studies of Antibacterial Peptidyl Derivatives Based upon the Binding Site of Human Cystatin C
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Sonochemical synthesis of rosuvastatin based novel 3-methyleneisoindolin-1-one derivatives as potential anticancer agents
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Synthesis and Thermal, Photophysical, Electrochemical Properties of 3,3-di[3-Arylcarbazol-9-ylmethyl]oxetane Derivatives
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Phthalocyanine Derivatives Possessing 2-(Morpholin-4-yl)ethoxy Groups As Potential Agents for Photodynamic Therapy
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Search for new tools to combat Gram-negative resistant bacteria among amine derivatives of 5-arylidenehydantoin
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Synthesis and biological evaluation of fluorinated 3-phenylcoumarin-7-O-sulfamate derivatives as steroid sulfatase inhibitors
PublicationIn the present work, we report the initial results of our study on a series of 3-phenylcoumarin sulfamate-based compounds containing C-F bonds as a novel inhibitors of steroid sulfatase (STS). The new compounds are potent STS inhibitors, possessing more than 10 times higher inhibitory potency than coumarin-7-O-sulfamate. In the course of our investigation, compounds 2b and 2c demonstrated the highest inhibitory effect in the enzymatic...
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Solid phase synthesis of 4,5,8-trihydroxy-9,10-anthraquinone-1-yl-(tuftsin or retro-tuftsin) derivatives
PublicationPrzedstawiono syntezę na fazie stałej połączeń leuko-1,4,5,8-tetra-hydroksyantrachinonów z pochodnymi tuftsyny i retro-tuftsyny zawierającymi wiązanie izopeptydowe. Do syntezy wykorzystano standardową metodę Fmoc i DIC jako odczynnik aktywujący.
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The antitumor derivatives, C1305 and C1748, were different in effects on CYP3A4 expression and catalytic activity in HepG2 cells
PublicationCytochromy P450 (CYP) należą do grupy enzymów biorących udział w 70-80% metabolizmu fazy I większości stosowanych klinicznie leków. Z tego powodu oddziaływanie leków z enzymami cytochromu P450 stało się istotnym elementem w projektowaniu chemoterapeutyków, szczególnie tych, które są stosowane w terapii wielolekowej. Znajomość substratów, induktorów i inhibitorów poszczególnych izoenzymów P450, nie tylko może obniżać częstość występowania...
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The Synthesis of 3-Amino-pyrazine-2-carbohydrazide and 3-Amino-N'-methylpyrazine-2-carbohydrazide Derivatives
PublicationW poszukiwaniu biologicznie aktywnych związków otrzymano szereg pochodnych 3-Amino-pirazyno-2-karbohydrazydu i 3-Amino-N'-metylopirazyno-2-karbohydrazydu w wyniku reakcji hydrazydu aminopirazynoinowegokwasu z izocyjanianami, aldehydami, ketonami, CS2 i kwasem mrówkowym.
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Chloroacridine derivatives as potential anticancer agents which may act as tricarboxylic acid cycle enzyme inhibitors
PublicationThe chloroacridines affect biological forms of melanoma in different ways. Amelanotic (Ab) melanoma (with inhibited melanogenesis and higher malignancy) was particularly sensitive to the action of the chloroacridines. The Ab melanoma cells died through apoptosis and through death without caspase activation. Diminished activity of TAC enzymes was noticed among Ab melanoma cells together with ATP/NAD depletion, especially in the...
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Influence of Osmolytes on Protein and Water Structure: A Step To Understanding the Mechanism of Protein Stabilization
PublicationResults concerning the thermostability of hen egg white lysozyme in aqueous solutions with stabilizing osmolytes, trimethylamine-N-oxide (TMAO), glycine (Gly), and its N-methyl derivatives, N-methylglycine (NMG), N,N-dimethylglycine (DMG), and N,N,N-trimethylglycine (betaine, TMG), have been presented. The combination of spectroscopic (IR) and calorimetric (DSC) data allowed us to establish a link between osmolytes’ influence on...
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Preliminary Microbiological Tests of S-Carvone and Geraniol and Selected Derivatives of These Compounds That May Be Formed in the Processes of Isomerization and Oxidation
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Adsorption of Hydrocarbon Chloro-Derivatives onto DTO Commercial Activated Carbon from Multi-Component Aqueous Solutions
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Anti-Helicobacter pylori activities of selected N-substituted cinnamamide derivatives evaluated on reference and clinical bacterial strains
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Nanoconjugates of graphene oxide derivatives and meso-tetraphenylporphyrin: a new avenue for anticancer photodynamic therapies – Cell-on-a-Chip analysis
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Photophysical properties of 3-[2-(N-phenylcarbazolyl)benzoxazol-5-yl]alanine derivatives – experimental and theoretical studies
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Density Functional Theory Studies on Ir Spectra of the Triphenylene Derivatives. A Scaled Quantum Mechanical Force Field Approach
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N-Substituted piperazine derivatives as potential multitarget agents acting on histamine H3 receptor and cancer resistance proteins
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Crystallographic studies of piperazine derivatives of 3-methyl-5-spirofluorenehydantoin in search of structural features of P-gp inhibitors
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Metabolism of antitumor 9-amino-1-nitroacridine derivatives in HepG2 cells and its influence on cytochrome P450 isoenzymes
PublicationCelem przeprowadzonych badań było określenie wpływu pochodnych C-857 i C-1748 na poziom enzymów cytochromu P450 w powiązaniu z kinetyką metabolizmu badanych związków. Eksperymenty zostały przeprowadzone na komórkach ludzkiego nowotworu wątroby HepG2. Uzyskane wyniki metodą Western blotting wykazały, że za metaboliczną transformacje pochodnych C-857 i C-1748 odpowiada izoenzym CYP3A4.Analiza metabolitów (Western blotting, HPLC)...