Design, synthesis and biological evaluation of deuterated nintedanib for improving pharmacokinetic properties. (26th May 2015)

• Record Type: Journal Article
• Authors: Xu, Ruixue; Zhan, Miao; Peng, Lingling; Pang, Xuehai; Yang, Jun; Zhang, Tao; Jiang, Hongxia; Zhao, Lifeng; Chen, Yuanwei
• Is Part Of: Journal of labelled compounds & radiopharmaceuticals. Volume 58:Number 7(2015)
• Page Start: 308
• Page End: 312
• Publication Date: 2015-05-26
• Subjects: Tracers (Chemistry) -- Periodicals; Radiopharmaceuticals -- Periodicals; 615.8424
• DOI: 10.1002/jlcr.3299
• Languages: English
• ISSNs: 0362-4803

Abstract

<abstract abstract-type="main"> <title> <x xml:space="preserve">Abstract</x> </title> <p>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 <italic>in vitro</italic> and <italic>in vivo</italic>. 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.</p> </abstract>