- Synthesis of diblock copolymers consisting of hyaluronan and poly(2-ethyl-2-oxazoline)
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The preparation of biomimetic diblock copolymers consisting of two hydrophilic units which include a nonionic block (PEtOz) and an anionic block (HA) was discussed. The amine-terminated poly(2-ethtyl-2-oxazolines) (NH 2PEtOz) was prepared using
- Yang, Yali,Kataoka, Kazunori,Winnik, Francoise M.
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- Extensive structure modification on luteolin-cinnamic acid conjugates leading to BACE1 inhibitors with optimal pharmacological properties
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BACE1 inhibitory conjugates derived from two natural products, luteolin (1) and p-hydroxy-cinnamic acid (2), were subjected to systematic structure modifications, including various positions in luteolin segment for conjugation, different linkers (length, bond variation), as well as various substitutions in cinnamic acid segment (various substituents on benzene, and replacement of benzene by heteroaromatics and cycloalkane). Optimal conjugates such as 7c and 7k were chosen on the basis of a series of bioassay data for further investigation.
- Sun, De-Yang,Cheng, Chen,Moschke, Katrin,Huang, Jian,Fang, Wei-Shuo
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supporting information
(2020/01/13)
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- Insights into the Pummerer synthesis of oxazolines
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A rapid and simple method to access unnatural 2-substituted 5-thio oxazolines has been developed. This methodology is based on a Pummerer reaction followed by an intramolecular nucleophilic substitution, which changes the paradigm for the normal use of a base in Pummerer chemistry. We also provide a useful two-step method for the synthesis of the starting material and a mechanistic proposal based on experimental observations, which contests the previously proposed reaction pathway. The reaction proved to be general, and different substituents, such as alkyl, aryl, alkenyl and functionalized groups, can be used without a significant decrease in efficiency.
- Becerra-Cely, Laura,Rueda-Espinosa, Juan,Ojeda-Porras, Andrea,Gamba-Sánchez, Diego
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p. 8474 - 8485
(2016/09/28)
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- A perylene diimide rotaxane: Synthesis, structure and electrochemically driven de-threading
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The first example of a [2]-rotaxane in which a perylene diimide acts as a recognition site has been synthesised and characterised. The interlocked nature of the compound has been verified by both NMR studies and an X-ray structure determination. Electroch
- Slater, Benjamin J.,Davies, E. Stephen,Argent, Stephen P.,Nowell, Harriott,Lewis, William,Blake, Alexander J.,Champness, Neil R.
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supporting information; experimental part
p. 14746 - 14751
(2012/02/14)
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- Synthesis, cytotoxicity, and insight into the mode of action of Re(CO) 3 thymidine complexes
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Nucleoside analogues are extensively used in the treatment of cancer and viral diseases. The antiproliferative properties of organorhenium(I) complexes, however, have been scarcely explored to date. Herein we present the syntheses, characterization, and in vitro evaluation of ReI(CO)3 core complexes of thymidine and uridine. For the binding of the Re I(CO)3 core, a tridentate dipicolylamine metal chelate was introduced at positions C5′, C2′, N3, and C5 with spacers of various lengths. The corresponding organometallic thymidine complexes were fully characterized by IR and NMR spectroscopy and mass spectrometry. Their cytotoxicity was assessed against the A549 lung carcinoma cell line. Toxicity is dependent on the site and mode of conjugation as well as on the nature and the length of the tether. Moderate toxicity was observed for conjugates carrying the rhenium moiety at position C5′ or N3 (IC50=124-160 μm). No toxicity was observed for complexes modified at C2′ or C5. Complex 53, with a dodecylene spacer at C5′, exhibits remarkable toxicity and is more potent than cisplatin, with an IC50 value of 6.0 μm. To the best of our knowledge, this is the first report of the antiproliferative properties of [M(CO)3]+1-nucleoside conjugates. In competitive inhibition experiments with A549 cell lysates and purified recombinant human thymidine kinase 1 (hTK-1), enzyme inhibition was observed for complexes modified at either N3 or C5′, but our results suggest that the toxicity cannot be attributed solely to interaction with hTK-1.
- Bartholomae, Mark D.,Vortherms, Anthony R.,Hillier, Shawn,Ploier, Birgit,Joyal, John,Babich, John,Doyle, Robert P.,Zubieta, Jon
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experimental part
p. 1513 - 1529
(2011/11/29)
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- Synthesis of N-(2-[18F]fluoroethyl)-N'-methylthiourea: A hydrogen peroxide scavenger
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N-(2-[18F]fluoroethyl)-N'-methylthiourea ([18F]FEMTU), a fluorine- 18 labelled derivative of the hydrogen peroxide scavenger dimethylthiourea (DMTU), has been synthesized by reaction of 2-[18F]fluoroethylamine with methyli
- Gilissen,Bormans,De Groot,Verbruggen
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p. 491 - 502
(2007/10/03)
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- N-(ω-TOSYLOXYALKYL)PHTHALIMIDES AS REACTIVE GENERAL SYNTHONS FOR INTRODUCING ALKYLAMINO GROUPS AND THEIR APPLICATION FOR THE "SELF-PROLIFERATIVE" SYNTHESIS OF OPEN-CHAIN POLYAMINES
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New synthetic routes to N-(ω-tosyloxyalkyl)phthalimides (2) were developed and the synthetic utility of 2 as alkylating reagents was exemplified in the open-chain polyamine synthesis involving the "self-proliferative" process.
- Iwata, Masaaki,Kuzuhara, Hiroyoshi
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p. 369 - 372
(2007/10/02)
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