Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 27, Issue 10, Pages 1932-1941Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2019.04.018
Keywords
FGFR4; Selectivity; Antitumor; Pharmacokinetic profile
Funding
- Jiangsu Province Hi-Tech Key Laboratory for Biomedical Research
- National Science and Technology Major Foundation of China
- State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources (Guangxi Normal University) [CMEMR2017-B05]
- Jiangsu Hansoh Pharmaceutical Corporation
- Priority Academic Program Development of Jiangsu Higher Education Institutions
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Total twenty-five 7-formyl-naphthyridyl-urea derivatives were designed, synthesized and evaluated for their inhibition of FGFR4 kinase and antitumor activity. The pharmacological data indicated that most of the tested compounds showed high selectivity towards FGFR4 kinase and could significantly inhibit FGFR4 and the tumor cells lines with the high expression of FGFR4. In particular, compounds 6f, 6g, 6h, 6l, 6m and 6s showed a good performance in pharmacokinetic tests. When tested in mice, the representative compound 6f was found to have good pharmacokinetic parameters, low toxicity, and better tumor inhibiting activity in vivo.
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