- Conjugated 5-fluorouracil with mitochondria-targeting lipophilic cation: Design, synthesis and biological evaluation
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5-Fluorouracil (5-FU) was linked with F16 by vulnerable bonds to selectively target cancer mitochondria which resulted in conjugated compounds, including F16-5-FU, F16-OOC-FU, F16-NHOC-FU and F16-SS-FU. F16-OOC-FU decreased the antiproliferative activity of 5-FU on the nontumor cell line, and the cytotoxicity of F16-SS-FU significantly increased when administered with dithiothreitol (DTT).
- Wang, Jia,Fan, Xiao-Yang,Yang, Li-Yun,He, Huan,Huang, Rong,Jiang, Feng-Lei,Liu, Yi
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Read Online
- Bis[3-(4′-substituted phenyl)prop-2-ene]disulfides as a new class of antihyperlipidemic compounds
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Novel derivatives of diallylsulfide, an active principle found in garlic, have been synthesized. The synthetic scheme, involving the Wittig reaction has been outlined. Among these derivatives, bis[3-(4′-nitrophenyl)prop-2-ene] disulfide has been found to be effective in lowering lipid levels and in inhibiting the activity of the enzyme HMG-CoA reductase, in Wistar rats. A series of bis[3-(4′-substituted phenyl)prop-2-ene]disulfides were prepared and their hypolipidemic activities were examined in hypercholesterolemic Wistar rats. Introduction of an electron withdrawing group to the phenyl ring in the parent compound led to the identification of compound 8 as a potent and efficacious hypolipidemic agent.
- Sharma, Meenakshi,Tiwari, Manisha,Chandra, Ramesh
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Read Online
- Gas chromatography/mass spectrometry analysis of reaction products of sulfur mustards with phenol
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Screening of chemicals related to chemical weapons convention including their all possible degradation and reaction products in environmental samples is important in the organization for prohibition of chemical weapons verification process. Sulfur mustards, commonly known as blistering agents, are included in schedule 1 chemicals of chemical weapons convention. Because of the presence of chlorine atoms in sulfur mustards, they are highly reactive and prone to react with other organic molecules such as phenols to produce corresponding reaction products. Thus, it is important to screen for not only the sulfur mustards but also their reaction products for verification process. The sulfur mustards and their degradation products have been routinely analyzed by gas chromatography/mass spectrometry method, however, the methods are yet to establish for the reaction products. In this study, the reaction products of the sulfur mustards with phenol (compounds 1–7) were studied by gas chromatography/mass spectrometry under electron ionization and chemical ionization conditions. The EI spectra of 1–7 displayed molecular ion and characteristic fragments that provided structure information. Mostly the fragment ions were due to homolytic cleavages involving C–O, C–S, and C–C cleavages. The methane or isobutane CI spectra showed M+., [M + H]+, and [M ? H]+ ions including reagent specific adduct ions. The CI spectra also showed other adduct ions formed by association of analyte molecule with its most abundant fragment ion. The gas chromatography/retention index values were also calculated, which support unambiguous identification of targeted molecules in suspected environmental samples. The method was demonstrated for detection of the targeted molecules spiked in soil samples.
- Prabhakar, S.,Reddy, T Jagadeshwar,Sandeep, M.,Srinivas, K.,Suresh Pal, A.,Veeresham, A.
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p. 213 - 224
(2019/11/22)
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- Mo-Based Oxidizers as Powerful Tools for the Synthesis of Thia- and Selenaheterocycles
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A highly efficient synthetic protocol for the synthesis of thia- and selenaheterocycles has been developed. By employing a MoCl5-mediated intramolecular dehydrogenative coupling reaction, a broad variety of structural motifs was isolated in yields up to 94 %. The electrophilic key transformation is tolerated by several labile moieties like halides and tertiary alkyl groups. Due to the use of disulfide or diselenide precursors, a high atom efficiency was achieved.
- Franzmann, Peter,Beil, Sebastian B.,Schollmeyer, Dieter,Waldvogel, Siegfried R.
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supporting information
p. 1936 - 1940
(2019/01/14)
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- Preparation method of high-purity mesna
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The invention belongs to the technical field of drug synthesis, and particularly relates to a preparation method of high-purity mesna. The invention provides a brand new synthetic thought of high-purity mesna. Since a sulfydryl compound is unstable, and a disulfide bond is likely to form, a main impurity (di-mesna) of mesna is firstly prepared, and finally the di-mesna is decomposed into mesna by virtue of conventional hydrogenation reduction, so that the process flow greatly reduces the content of the di-mesna in the mesna, the reaction raw materials are easy to obtain, the operation is simple, the yield and purity are greatly increased, and the preparation method is suitable for the industrialized production.
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Paragraph 0037; 0038; 0039; 0046; 0052
(2017/10/22)
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- Potent haloperidol derivatives covalently binding to the dopamine D2 receptor
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The dopamine D2 receptor (D2R) is a common drug target for the treatment of a variety of neurological disorders including schizophrenia. Structure based design of subtype selective D2R antagonists requires high resolution crystal structures of the receptor and pharmacological tools promoting a better understanding of the protein-ligand interactions. Recently, we reported the development of a chemically activated dopamine derivative (FAUC150) designed to covalently bind the L94C mutant of the dopamine D2 receptor. Using FAUC150 as a template, we elaborated the design and synthesis of irreversible analogs of the potent antipsychotic drug haloperidol forming covalent D2R-ligand complexes. The disulfide- and Michael acceptor-functionalized compounds showed significant receptor affinity and an irreversible binding profile in radioligand depletion experiments.
- Schwalbe, Tobias,Kaindl, Jonas,Hübner, Harald,Gmeiner, Peter
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p. 5084 - 5094
(2017/09/26)
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- Nanoparticles and nanoparticle compositions
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The invention provides multivalent surface-crosslinked micelle (SCM) particles, crosslinked reverse micelle (CRM) particles, and methods of making and using them. The SCM particles can be used, for example, to inhibit a virus or bacteria from binding to a host cell. The inhibition can be used in therapy for the flu, cancer, or AIDS. The CRM particles can be used, for example, to prepare metal nanoparticles or metal alloy nanoparticles, or they can be used in catalytic reactions.
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Page/Page column 54
(2016/06/01)
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- NANOPARTICLES AND NANOPARTICLE COMPOSITIONS
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The invention provides multivalent surface-crosslinked micelle (SCM) particles, crosslinked reverse micelle (CRM) particles, and methods of making and using them. The SCM particles can be used, for example, to inhibit a virus or bacteria from binding to a host cell. The inhibition can be used in therapy for the flu, cancer, or AIDS. The CRM particles can be used, for example, to prepare metal nanoparticles or metal alloy nanoparticles, or they can be used in catalytic reactions.
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Paragraph 0252; 0253
(2013/05/08)
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- Rapid release of entrapped contents from multi-functionalizable, surface cross-linked micelles upon different stimulation
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Hydrophobic guests such as pyrene could be readily trapped inside the micelles of an alkynylated surfactant in the presence of an azide-functionalized cross-linker using the click reaction. The cross-linker was designed to contain cleavable bonds such as geminal diol, disulfide, and acetal. The resulting pyrene-containing water-soluble nanoparticle was under electrostatic stress when diluted below the CMC of the surfactant. Extremely rapid (1 min) release of the hydrophobic content was observed when the cross-linker was cleaved. This method combines the ease of physical entrapment and the precision of chemical ligation, and potentially is highly useful in the delivery and controlled release of pharmaceutical agents.
- Zhang, Shiyong,Zhao, Yan
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supporting information; experimental part
p. 10642 - 10644
(2010/11/05)
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- Synthesis, DNA binding, and cytotoxic evaluation of new analogs of diallyldisulfide, an active principle of garlic
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Diallyldisulfide (DADS), an active principle of garlic (Allium sativum) is known for its antihyperlipidemic properties. However, its use is limited due to its extreme volatility. In the present study, we have synthesized and characterized a series of six
- Rai, Santosh Kumar,Sharma, Meenakshi,Tiwari, Manisha
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p. 7302 - 7310
(2008/12/23)
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- Prodrugs containing novel bio-cleavable linkers
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The invention provides the compounds of formula (I) or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutical compositions comprising one or more compounds of formula I or intermediates thereof and one more of pharmaceutically acceptable carriers, vehicles or diluents. The invention further provides methods of preparation and methods of use of prodrugs including NO-releasing prodrugs, double prodrugs and mutual prodrugs comprising the compounds of formula I.
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Page/Page column 113; 131
(2008/06/13)
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- DIALLYLDISULPHIDE COMPOUNDS HAVING ANTILIPIDEMIC AND ANTIOXIDANT ACTIVITY
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The present invention relates to a novel diallyldisulphide derivative having formula I as shown herebelow and their pharmaceutically acceptable salts; R-CH = CH - CH2-S-S-CH2-CH = CH-R (Formula I)wherein R=C6HnX
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- Inhibitors of phospholipase enzymes
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This invention provides substituted indole and indoline compounds useful in inhibiting phospholipase activity, particularly including cytosolic phospholipase A2 (cPLA2) activity, as well as pharmaceutical compositions containing the compounds and methods of using them to treat various maladies, including pain and inflammatory conditions.
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- Studies on the Formation of Dihydro-1,4-oxathiines by Halogenation of 1,3-Oxathiolanes.
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Formation of 5,6-dihydro-1,4-oxathiines (1a-g) by halogenation of 1,3-oxathiolanes (4a-g) was investigated.Moderate yields of (1) were obtained in systems in which the newly formed double bond of the heterocyclic ring was stabilised by conjugation.In addition to the dihydro-1,4-oxathiines (1a-g), their halogenated derivatives and some fused and spiro 1,4-oxathianes were produced as by-products.By-products of reactions were analysed by gas chromatography and mass-spectrometry.
- Nevalainen, Vesa,Pohjala, Esko
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p. 1401 - 1421
(2007/10/02)
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