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

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

  • Bioorg Med Chem. 2010 Mar 15;18(6):2317-2326. doi: 10.1016/j.bmc.2010.01.051.
M V Ramana Reddy 1,  Venkat R Pallela 1,  Stephen C Cosenza 1,  Muralidhar R Mallireddigari 2,  Revathi Patti 2,  Marie Bonagura 1,  May Truongcao 1,  Balaiah Akula 2,  Shashidhar S Jatiani 1,  E Premkumar Reddy 1
Affiliations

Affiliations

  • 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.
PMID: 20188579 DOI: 10.1016/j.bmc.2010.01.051
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.

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