86855-27-8Relevant academic research and scientific papers
N6-benzyladenosine derivatives as novel n-donor ligands of platinum(ii) dichlorido complexes
Starha, Pavel,Popa, Igor,Travnicek, Zdenek,Vanco, Jan
, p. 6990 - 7003 (2013/07/26)
The platinum(II) complexes trans-[PtCl2(Ln)2]·xSolv 1-13 (Solv = H2O or CH3OH), involving N6-benzyladenosine-based N-donor ligands, were synthesized; Ln stands for N6-(2-methoxybenzyl)adenosine (L1, involved in complex 1), N6-(4-methoxybenzyl) adenosine (L2, 2), N6-(2-chlorobenzyl)adenosine (L3, 3), N6-(4-chlorobenzyl)- adenosine (L4, 4), N6-(2-hydroxybenzyl)adenosine (L5, 5), N6-(3-hydroxybenzyl)- adenosine (L6, 6), N6-(2-hydroxy-3-methoxybenzyl) adenosine (L7, 7), N6-(4-fluorobenzyl) adenosine (L8, 8), N6-(4-methylbenzyl) adenosine (L9, 9), 2-chloro-N6-(3-hydroxybenzyl) adenosine (L10, 10), 2-chloro-N6-(4-hydroxybenzyl)adenosine (L11, 11), 2-chloro- N6-(2-hydroxy-3- methoxybenzyl)adenosine (L12, 12) and 2-chloro-N6-(2-hydroxy-5- methylbenzyl)adenosine (L13, 13). The compounds were characterized by elemental analysis, mass spectrometry, IR and multinuclear (1H-, 13C-, 195Pt- and 15N-) and two-dimensional NMR spectroscopy, which proved the N7-coordination mode of the appropriate N6-benzyladenosine derivative and trans-geometry of the title complexes. The complexes 1-13 were found to be non-toxic in vitro against two selected human cancer cell lines (HOS and MCF7; with IC50 > 50.0 μM). However, they were found (by ESI-MS study) to be able to interact with the physiological levels of the sulfur-containing biogenic biomolecule L-methionine by a relatively simple 1:1 exchange mechanism (one Ln molecule was replaced by one L-methionine molecule), thus forming a mixed-nitrogen/sulfur-ligand dichlorido-platinum(II) coordination species.
Characterization of scavengers of γ-ketoaldehydes that do not inhibit prostaglandin biosynthesis
Zagol-Ikapitte, Irene,Amarnath, Venkataraman,Bala, Manju,Roberts II, L. Jackson,Oates, John A.,Boutaud, Olivier
scheme or table, p. 240 - 250 (2011/02/22)
Expression of cyclooxygenase-2 (COX-2) is associated with the development of many pathologic conditions. The product of COX-2, prostaglandin H2 (PGH2), can spontaneously rearrange to form reactive γ-ketoaldehydes called levuglandins (LGs). This γ-ketoaldehyde structure confers a high degree of reactivity on the LGs, which rapidly form covalent adducts with primary amines of protein residues. Formation of LG adducts of proteins has been demonstrated in pathologic conditions (e.g., increased levels in the hippocampus in Alzheimer's disease) and during physiologic function (platelet activation). On the basis of knowledge that lipid modification of proteins is known to cause their translocation and to alter their function, we hypothesize that modification of proteins by LG could have functional consequences. Testing this hypothesis requires an experimental approach that discriminates between the effects of protein modification by LG and the effects of cyclooxygenase-derived prostanoids acting through their G-protein coupled receptors. To achieve this goal, we have synthesized and evaluated a series of scavengers that react with LG with a potency more than 2 orders of magnitude greater than that with the ε-amine of lysine. A subset of these scavengers are shown to block the formation of LG adducts of proteins in cells without inhibiting the catalytic activity of the cyclooxygenases. Ten of these selective scavengers did not produce cytotoxicity. These results demonstrate that small molecules can scavenge LGs in cells without interfering with the formation of prostaglandins. They also provide a working hypothesis for the development of pharmacologic agents that could be used in experimental animals in vivo to assess the pathophysiological contribution of levuglandins in diseases associated with cyclooxygenase up-regulation.
Arylalkylamine vanadium (V) salts for the treatment and/or prevention of Diabetes mellitus
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Page/Page column 17, (2010/11/26)
This invention provides compounds of formula (IIA) and pharmaceutical compositions thereof, where M, a, b, and R1-R5 are as defined herein, for treating human type 1 and type 2 diabetes, particularly insulin-resistant diabetes. Pharmaceutical compositions comprising the compounds of formula (IIA) are also disclosed.
ARYLALKYLAMINE VANADIUM (V) SALTS FOR THE TREATMENT AND/OR PREVENTION OF DIABETES MELLITUS
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Page/Page column 41-42, (2010/02/15)
This invention provides compounds and pharmaceutical compositions thereof for treating human type 1 and type 2 diabetes, particularly insulin-resistant diabetes.
COMPOSITION OF SSAO SUBSTRATES AND METAL COMPOUNDS OF THE VLA AND VLB GROUPS OF THE PERIODIC TABLE
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Page/Page column 23, (2010/11/08)
This invention relates to (pharmaceutical) compositions comprising a combination of SSAO substrates and pharmaceutically acceptable compounds of the Vla and Vlb group of the periodic table, i.e. selenium (VI)-, molybdenum (VI)- and tungsten (V)/(VI) compounds, etc. and to their use as insulin mimetic, i.e., to treat illness Diabetes mellitus, Obesity, or their symptoms. A here discovered synergism between the compounds of the Vla and Vlb groups of the periodic table, i.e. selenium (VI)-, molybdenum (VI)- and tungsten (V)/(VI) com-pounds, etc. and the SSAO substrates makes the effective concentration of the compounds of the Via and Vlb groups of the periodic table in the (pharmaceutical) composition one order of magnitude lower than the corresponding compound of the Vla and Vlb groups alone. Consequently the inventive (pharmaceutical) composition has much lower toxicity than the known compounds or compositions in the art alone, what is a crucial advantage of the former for its use in the treatment and/or prevention of Diabetes mellitus, particularly of Diabetes type 2, or Obesity.
SUBSTITUTED PYRIMIDINES
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Page/Page column 26, (2008/06/13)
The invention relates to novel substituted pyrimidines of formula (I), in which R1, R2, R3, R4, Q, X and n have the meanings as cited in the description. The invention also relates to a method and intermediate products for producing these pyrimidines, and to the use thereof as plant control agents, particularly as herbicides.
