期刊
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS
卷 58, 期 7, 页码 308-312出版社
WILEY
DOI: 10.1002/jlcr.3299
关键词
Nintedanib; triple angiokinase inhibitor; deuterium isotope effect; antitumor activity
资金
- National Natural Science Foundation of China [81472418]
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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