Search results for: THIOPHOSPHATE
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Phosphate and Thiophosphate Biphenyl Analogs as Steroid Sulfatase Inhibitors
PublicationIn the present work, we report convenient methods for the synthesis and biological evaluation of phosphate and thiophosphate biphenyl derivatives exhibiting steroid sulfatase (STS) activity. The described synthesis is based on straightforward preparation of biphenyl-4-ol and 40-hydroxybiphenyl- 4-carboxylic acid ethyl ester modified with various phosphate or thiophosphate moieties. The inhibitory effects of these compounds were...
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Synthesis of bicoumarin thiophosphate derivatives as steroid sulfatase inhibitors
PublicationBased on the frameworks of 7-hydroxy-2,3-dihydro-1H-cyclopenta[c]chromen-4-one, 3-hydroxy- 7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one and 3-hydroxy-8,9,10,11-tetrahydro-7H-cyclohepta[c] chromen-6-one, a series of bicoumarin thiophosphate analogs have been synthesized and biologically evaluated. Additionally, their binding modes have been modeled using docking techniques. The inhibitory properties of the synthesized compounds...
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Steroid Sulfatase Inhibitors Based on Phosphate and Thiophosphate Flavone Analogs
PublicationA series of phosphate and thiophosphate flavone derivatives were synthesized and biologically evaluated in vitro for inhibition of steroid sulfatase (STS) activity. The described synthesis includes the straightforward preparation of 7-hydroxy-2-phenyl-4H-chromen-4-one 3a, 2-(4-fluorophenyl)-7-hydroxy-4H-chromen-4-one 3b, 7-hydroxy-2-(4-(trifluoromethyl)phenyl)-4H-chromen-4-one 3c, 7-hydroxy-2-(p-tolyl)-4H-chromen-4-one 3d modified...
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Synthesis and biological evaluation of thiophosphate tricyclic coumarin derivatives as steroid sulfatase inhibitors
PublicationSteroid sulfatase (STS) enzyme inhibition is an important approach to the management of hormone-dependent breast cancer. In this paper, we report convenient methods for the synthesis and biological evaluation of thiophosphate tricyclic coumarin analogs exhibiting STS activity. The described methods are based on the straightforward preparation of 7-hydroxy-2,3-dihydro-1H-cyclopenta[c]chromen-2-one, 3-hydroxy- 7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one,...
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Synthesis and steroid sulfatase inhibitory activities of N-alkanoyl tyramine phosphates and thiophosphates
PublicationA series of phosphate and thiophosphate analogs based on the frameworks of N-alkanoyl tyramines have been synthesized and biologically evaluated. Their binding modes have been modeled using docking techniques. The inhibitory effects of the synthesized compounds were tested on STS isolated from the human placenta as well as the MCF-7, MDA-MB-231 and SkBr3 cancer cell lines. Most of the new STS inhibitors possessed potent activity...
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Unexpected thioketene derivative formation during thioacyl dithiophosphate synthesis.
PublicationZbadano zakres i ograniczenia tioacylowania opartego na ditiofosforanach tioacylu. Ditiofosforany tioacylo otrzymano w wyniku reakcji ditiofosforanów acylu z kwasem ditiofosforowym. Obecność dwóch podstawników w pozycji alfa we fragmencie acylowym faworyzowała tworzenie pochodnych tioketenu tym samym obniżając wydajność oczekiwanych ditiofosforanów tioacylu.
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Adenosine triphosphate in the marine boundary layer in the southern Baltic Sea
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Ammonium <i>O</i>,<i>O</i>'-diethyl dithiophosphate
PublicationIn the title compound, NH4+·(C2H5O)2PS2−, the ammonium cation is connected by four charge-assisted N−H···S hydrogen bonds to four tetrahedral O,O'-diethyl dithiophosphate anions, forming layers parallel to (100). The polar and non-polar constituents of the layers are stacked alternately along [100]. Interlacing of the external ethyl groups...
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A novel nucleotide found in human erythrocytes, 4-pyridone-3-carboxamide-1-beta-D-ribonucleoside triphosphate
PublicationZidentyfikowano nowy, nieznany nukleotyd, występujący w erytrocytach osób chorych na przewlekłą niewydolność nerek, w stężeniu porównywalnym do zawartości ATP. Nukleotyd ten wyizolowano chromatograficznie, a jego strukturę określono jako trójfosforan 4-piridono-3-karboksyamido-1-b-D-rybonukleozydu, na podstawie danych spektralnych UV, MS, IR i NMR.
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Mechanism of reaction of RNA-dependent RNA polymerase from SARS-CoV-2
PublicationWe combine molecular dynamics, statistical mechanics, and hybrid quantum mechanics/molecular mechanics simulations to describe mechanistically the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) RNA-dependent RNA polymerase (RdRp). Our study analyzes the binding mode of both natural triphosphate substrates as well as remdesivir triphosphate (the active form of drug), which is bound preferentially over ATP by RdRp while...
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(4-(Bis(4-Fluorophenyl)Methyl)Piperazin-1-yl)(Cyclohexyl)Methanone Hydrochloride (LDK1229): A New Cannabinoid CB1 Receptor Inverse Agonist from the Class of Benzhydryl Piperazine Analogs
PublicationSome inverse agonists of cannabinoid receptor type 1 (CB1) have been demonstrated to be anorectic antiobesity drug candidates. However, the first generation of CB1 inverse agonists, represented by rimonabant (SR141716A), otenabant, and taranabant, are centrally active, with a high level of psychiatric side effects. Hence, the discovery of CB1 inverse agonists with a chemical scaffold distinct from these holds promise for developing...
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Modyfikacja cementu kostnego w celu uzyskania długotrwałej ochrony antybakteryjnej
PublicationNiniejsza rozprawa doktorska stanowi przewodnik po jednotematycznym cyklu publikacji, dotyczącym modyfikacji akrylowego cementu kostnego celem uzyskania długotrwałej i efektywnej ochrony antybakteryjnej. W ramach niego przeprowadzono badania eksperymentalne polegające na opracowaniu technologii wytwarzania modyfikowanego cementu kostnego oraz procedury medycznej jego stosowania. Cement kostny był modyfikowany przez zastosowanie...
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Green porous benzamide-like nanomembranes for hazardous cations detection, separation, and concentration adjustment
PublicationGreen biomaterials play a crucial role in the diagnosis and treatment of diseases as well as health-related problem-solving. Typically, biocompatibility, biodegradability, and mechanical strength are requirements centered on biomaterial engineering. However, in-hospital therapeutics require an elaborated synthesis of hybrid and complex nanomaterials capable of mimicking cellular behavior. Accumulation of hazardous cations like...