Journal
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS
Volume 58, Issue 7, Pages 308-312Publisher
WILEY
DOI: 10.1002/jlcr.3299
Keywords
Nintedanib; triple angiokinase inhibitor; deuterium isotope effect; antitumor activity
Funding
- National Natural Science Foundation of China [81472418]
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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.
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