- Design, synthesis and evaluation of (E)-α-benzylthio chalcones as novel inhibitors of BCR-ABL kinase
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Novel (E)-α-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.
- Reddy, M.V. Ramana,Pallela, Venkat R.,Cosenza, Stephen C.,Mallireddigari, Muralidhar R.,Patti, Revathi,Bonagura, Marie,Truongcao, May,Akula, Balaiah,Jatiani, Shashidhar S.,Reddy, E. Premkumar
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experimental part
p. 2317 - 2326
(2010/05/17)
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- SULFIDE, SULFOXIDE AND SULFONE CHALCONE ANALOGUES, DERIVATIVES THEREOF AND THERAPEUTIC USES THEREOF
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Compounds useful as antiproliferative agents according to formula (I): wherein Ar1, Ar2, Ar3, m and n are as defined herein, salts, antibody conjugates, pharmaceutical compositions, methods of treatment, and synthetic methods are provided.
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Page/Page column 73; 90
(2008/12/06)
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