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Chem Biol Drug Des. 2017 Mar;89(3):420-427. doi: 10.1111/cbdd.12863. Epub 2016 Oct 17.

Synthesis and biological evaluation of novel dasatinib analogues as potent DDR1 and DDR2 kinase inhibitors.

Author information

1
Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, Guangzhou, China.
2
University of Chinese Academy of Sciences, Beijing, China.
3
State Key Laboratory of Respiratory Diseases, Guangzhou Medical University, Guangzhou, China.

Abstract

Novel dasatinib analogues as DDR1 and DDR2 inhibitors were designed and synthesized. The synthesized compounds were screened for DDR1 and DDR2 kinase inhibitory and cancer cell proliferation inhibitory activities. Some of the compounds showed the potent inhibitory activities against both DDR1 and DDR2, as well as anticancer activity in low nanomolar range against K562 cell line; especially, compound 3j demonstrated significantly better inhibitory potency than the parental dasatinib against both DDRs and also demonstrated the potent inhibitory activity against K562 cell lines (IC50 values of 2.26±0.46 nm for DDR1, 7.04±2.90 nm for DDR2, and 0.125±0.017 nm for K562 cell line).

KEYWORDS:

DDR1; DDR2; anticancer activity; dasatinib; kinase inhibitor

PMID:
27589335
DOI:
10.1111/cbdd.12863
[Indexed for MEDLINE]

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