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Your search keyword '"Xu, Ruixue"' showing total 2 results
Start Over Author "Xu, Ruixue" Topic deuterium
2 results on '"Xu, Ruixue"'

1. Design, synthesis and biological evaluation of deuterated nintedanib for improving pharmacokinetic properties.

Author

Xu R, Zhan M, Peng L, Pang X, Yang J, Zhang T, Jiang H, Zhao L, and Chen Y

Subjects
Animals, Antineoplastic Agents chemical synthesis, Indoles chemical synthesis, Isotope Labeling, Mice, Mice, Inbred BALB C, Tissue Distribution, Antineoplastic Agents pharmacokinetics, Deuterium chemistry, Indoles pharmacokinetics
Abstract

Nintedanib is a novel triple angiokinase inhibitor that inhibits three growth factors simultaneously. Deuterated derivatives of nintedanib at certain metabolically active sites were prepared and evaluated in vitro and in vivo. In particular, deuterated compound SKLB-C2202 had significantly improved pharmacokinetic properties compared with nintedanib. These efforts lay the foundation for further investigating the druggability of SKLB-C2202., (Copyright © 2015 John Wiley & Sons, Ltd.)

Published
2015
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2. A Simple and Cost-Effective Method for the Regioselective Deuteration of Phenols.

Author

Zhan, Miao, Xu, Ruixue, Tian, Ye, Jiang, Hongxia, Zhao, Lifeng, Xie, Yongmei, and Chen, Yuanwei

Subjects
*DEUTERIUM, *REGIOSELECTIVITY (Chemistry), *AROMATIC compounds, *SUBSTITUTION reactions, *PHENOLS
Abstract

A highly effective and operationally simple method for the deuteration of phenols using NaOH as a catalyst and D2O as the deuterium source is presented. A high regioselectivity for the ortho and/or para hydrogens relative to the oxygen atom was achieved, as well as a high degree of deuterium incorporation. The method also has a high functional-group tolerance, and allowed the deuteration of complex pharmaceutically interesting substrates. [ABSTRACT FROM AUTHOR]

Published
2015
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