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Bioorg Med Chem. 2010 Mar 15;18(6):2317-2326. doi: 10.1016/j.bmc.2010.01.051. Epub 2010 Jan 25.

Design, synthesis and evaluation of (E)-alpha-benzylthio chalcones as novel inhibitors of BCR-ABL kinase.

Author information

1
Fels Institute for Cancer Research and Molecular Biology, Temple University School of Medicine, 3307 North Broad Street, Philadelphia, PA 19140-5101, United States.
2
Onconova Therapeutics Inc., 375 Pheasant Run, Newtown, PA 18940, United States.

Abstract

Novel (E)-alpha-benzylthio chalcones are reported with preliminary in vitro activity data indicating that several of them are potent inhibitors (comparable to imatinib, the reference compound) of BCR-ABL phosphorylation in leukemic K562 cells, known to express high levels of BCR-ABL. The ability of such compounds to significantly inhibit K562 cell proliferation suggests that this scaffold could be a promising lead for the development of anticancer agents that are able to block BCR-ABL phosphorylation in leukemic cells.

PMID:
20188579
DOI:
10.1016/j.bmc.2010.01.051
[Indexed for MEDLINE]

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