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Design, synthesis and biological evaluation of deuterated nintedanib for improving pharmacokinetic properties
Author(s) -
Xu Ruixue,
Zhan Miao,
Peng Lingling,
Pang Xuehai,
Yang Jun,
Zhang Tao,
Jiang Hongxia,
Zhao Lifeng,
Chen Yuanwei
Publication year - 2015
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.3299
Subject(s) - chemistry , pharmacokinetics , deuterium , nintedanib , pharmacology , combinatorial chemistry , biochemical engineering , chromatography , medicine , nuclear physics , physics , idiopathic pulmonary fibrosis , engineering , lung
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.