Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 63, Issue -, Pages 702-712Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2013.03.013
Keywords
Dasatinib; Tyrosine kinase; Cytotoxic activity; Cancer cell; quinazolines; CML
Categories
Funding
- National Basic Research Program of China [2011CB933503]
- Technology Supporting Program of Jiangsu province [BE2009639, BE2012657]
Ask authors/readers for more resources
Three series of novel 4-benzothiazole amino quinazolines Dasatinib derivatives have been designed and synthesized. The entire target compounds were investigated for their in vitro cytotoxic activity by the MTT-based assay against 6 human cancer cell lines. Compared with the parental Dasatinib, most of the new compounds, especially 2, 4, 6-trimethylaniline series (3), demonstrated significant inhibitory activities against six cell lines. Furthermore, the target compounds were screened for Src and Abl kinase inhibitory activity. Among them, 1a, 1f and 3a-3f are more potential dual Src/Abl kinase inhibitors. Thus they may be promising lead compounds to be developed as an alternative for current Dasatinib therapy or for Imatinib-resistant patients, potentially via simultaneously blocking multiple RTK signaling pathways. (c) 2013 Elsevier Masson SAS. All rights reserved.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available