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Bioorg Med Chem Lett. 2012 Jan 15;22(2):806-10. doi: 10.1016/j.bmcl.2011.12.070. Epub 2011 Dec 20.

Design, synthesis, and in vitro antiproliferative activity of novel Dasatinib derivatives.

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1
School of Chemistry and Chemical Engineering, Institute of Pharmaceutical Engineering, Southeast University, 87 Dingjiaqiao, Nanjing, Jiangsu 210096, PR China.

Abstract

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 (1)H NMR and (13)C NMR.

PMID:
22217877
DOI:
10.1016/j.bmcl.2011.12.070
[Indexed for MEDLINE]
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