Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 22, Issue 2, Pages 806-810Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.12.070
Keywords
Dasatinib; Tyrosine kinase; Cytotoxic activity; Cancer cell
Categories
Funding
- National Basic Research Program of China [2011CB933503]
- Technology Supporting Program of Jiangsu province [BE2009639]
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Two series of novel Dasatinib derivatives have been designed and synthesized, with their in vitro cytostatic effect screened on human chronic myeloid leukemia cell line K562 and human myeloid leukemia cell line U937. Some target compounds demonstrated significant inhibitory activities against both cell lines. Compared to the contrast drug Dasatinib, 1b, 1c, 1d, 1e and 1f were found to demonstrate more potent antitumor activities. The structures of all the newly synthesized compounds were determined by H-1 NMR and C-13 NMR. (C) 2011 Elsevier Ltd. All rights reserved.
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