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
  • 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.