- Tuning the DNA binding and cleavage of bpa Cu(II) complexes by ether tethers with hydroxyl and methoxy groups
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Five bpa (bis(2-picolyl)amine) derivatives (1b, 2e, 3f, 4c, 5d) carrying ether tethers with hydroxyl and methoxy groups, have been synthesized from pyridine aldehyde and the respective amines by reductive amination. Their Cu(II) complexes carrying additio
- Sudarga Tjakraatmadja, Airlangga Arya Janitra,Lüdtke, Carsten,Kulak, Nora
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- Inhibition of Herpes Simplex Virus Type 1 Attachment and Infection by Sulfated Polyglycerols with Different Architectures
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Inhibition of herpes simplex virus type 1 (HSV-1) binding to the host cell surface by highly sulfated architectures is among the promising strategies to prevent virus entry and infection. However, the structural flexibility of multivalent inhibitors plays a major role in effective blockage and inhibition of virus receptors. In this study, we demonstrate the inhibitory effect of a polymer scaffold on the HSV-1 infection by using highly sulfated polyglycerols with different architectures (linear, dendronized, and hyperbranched). IC50 values for all synthesized sulfated polyglycerols and the natural sulfated polymer heparin were determined using plaque reduction infection assays. Interestingly, an increase in the IC50 value from 0.03 to 374 nM from highly flexible linear polyglycerol sulfate (LPGS) to less flexible scaffolds, namely, dendronized polyglycerol sulfate and hyperbranched polyglycerol sulfate was observed. The most potent LPGS inhibits HSV-1 infection 295 times more efficiently than heparin, and we show that LPGS has a much reduced anticoagulant capacity when compared to heparin as evidenced by measuring the activated partial thromboplastin time. Furthermore, prevention of infection by LPGS and the commercially available drug acyclovir were compared. All tested sulfated polymers do not show any cytotoxicity at concentrations of up to 1 mg/mL in different cell lines. We conclude from our results that more flexible polyglycerol sulfates are superior to less flexible sulfated polymers with respect to inhibition of HSV-1 infection and may constitute an alternative to the current antiviral treatments of this ubiquitous pathogen.
- Pouyan, Paria,Nie, Chuanxiong,Bhatia, Sumati,Wedepohl, Stefanie,Achazi, Katharina,Osterrieder, Nikolaus,Haag, Rainer
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- Multihydroxyl-functional polystyrenes in continuous flow
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We describe the synthesisof end-functionalized polystyrenes byliving anionic polymerization ina microstructured reactor via termination by acetal-protected functional epoxides. Initiation of styrene polymerization by alkyllithium takes place in a micromix
- Tonhauser, Christoph,Wilms, Daniel,Wurm, Frederik,Berger-Nicoletti, Elena,Maskos, Michael,Lowe, Holger,Frey, Holger
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experimental part
p. 5582 - 5588
(2011/10/12)
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- An efficient and stereoselective synthesis of (2R,2′S)-1-O-(2′-hydroxyhexadecyl)glycerol and its oxo analogs: Potential antitumour compounds from Shark Liver Oil
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Reproducible, high-yielding, cost efficient, regio- and stereoselective synthesis of the title compound 3 isolated from Shark Liver Oil has been described. The compound 3 is prepared in an overall yield of 41% from chiral synthon 4 by the sequential reaction of 4 with C-13 Wittig salt; hydrogenation; epoxidation and regioselective opening. The oxo analogs 18 and 19 are prepared from four different achiral synthons by the sequential regioselective opening of the corresponding epoxide with different alcohols, methylation and deprotection strategies. Copyright
- Baskaran, Subramanian,Baig, Mirza Hamed A.,Banerjee, Sharmila,Baskaran, Chitra,Bhanu, Kanchinadham,Deshpande, Sonali P.,Trivedi, Girish K.
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p. 6437 - 6452
(2007/10/03)
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- Fluorine-containing nitroazole derivatives and radiosensitizer comprising the same
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A nitroazole derivative of the formula: wherein NA is 3-nitro-1,2,4-triazol-l-yl and Rf is a fluorine-containing organic group which is useful as a radiosensitizer.
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- Fluorine-containing 2-nitroimidazole derivatives
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A 2-nitroimidazole derivative of the formula: STR1 wherein Rf is a group of the following formula (II) or (III): wherein X is a hydrogen atom or a halogen atom; R1 is a group of the formula: STR2 wherein R2 is a hydrogen a
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