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941.
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Andreas Faust Nicole Bumer Alina Schlütermann Manuel Becht Lilo Greune Christiane Geyer Christian Rüter Renato Margeta Lisa Wittmann Petra Dersch Georg Lenz Wolfgang E. Berdel Sebastian Bumer 《Angewandte Chemie (International ed. in English)》2022,61(1):e202109769
Ibrutinib is an inhibitor of Bruton's tyrosine kinase that has been approved for the treatment of patients with chronic lymphocytic leukemia, mantle cell lymphoma and Waldenstrom's macroglobulinemia and is connected with toxicities. To minimize its toxicities, we linked ibrutinib to a cell-targeted, internalizing antibody. To this end, we synthesized a poly-anionic derivate, ibrutinib-Cy3.5, that retains full functionality. This anionic inhibitor is complexed by our anti-CD20-protamine targeting conjugate and free protamine, and thereby spontaneously assembles into an electrostatically stabilized vesicular nanocarrier. The complexation led to an accumulation of the drug driven by the CD20 antigen internalization to the intended cells and an amplification of its pharmacological effectivity. In vivo, we observed a significant enrichment of the drug in xenograft lymphoma tumors in immune-compromised mice and a significantly better response to lower doses compared to the original drug. 相似文献
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Cover Picture: Influence of Polymer Electronics on Selective Dispersion of Single‐Walled Carbon Nanotubes (Chem. Eur. J. 41/2016) 下载免费PDF全文
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Austin R. Leise Nicole Comas Doug Harrison Dipak Patel Eileen G. Whitemiller Jennifer Wilson Jacob Timms Ian Golightly Christopher G. Hamaker Shawn R. Hitchcock 《Tetrahedron: Asymmetry》2017,28(9):1154-1162
An N4-p-methoxybenzyloxadiazinone has been prepared from (1R,2S)-norephedrine through a process of reductive amination, N-nitrosation, reduction, and cyclization. The oxadiazinone was acylated and employed in the asymmetric aldol addition reaction with aromatic and aliphatic aldehydes to yield aldol adducts in isolated yields ranging from 54% to 90%. Selected aldol adducts were treated with ceric ammonium nitrate in aqueous acetonitrile to afford the desired β-hydroxycarboxylic acids through a tandem process of oxidative cleavage of the N4-p-methoxybenzyl group and acidic hydrolysis of the N3-acyl side chain. The β-hydroxycarboxylic acids were recovered in high diastereomeric purity as determined by 500 MHz 1H NMR spectroscopy and the absolute configuration was confirmed by polarimetry. The chiral auxiliary unit, the 3,4,5,6-tetrahydro-2H-1,3,4-oxadiazin-2-one (oxadiazinone), was converted into its corresponding 3,6-dihydro-2H-1,3,4-oxadiazin-2-one (oxadiazinone) through an oxidative pathway promoted by the ceric ammonium nitrate. 相似文献
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Biological evaluation of 1,2,3‐triazole‐based polymers for potential applications as hard tissue material 下载免费PDF全文
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