title: Design, synthesis and evaluation of (E)-alpha-benzylthio chalcones as novel inhibitors of BCR-ABL kinase.
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.
authors.affiliation: Fels Institute for Cancer Research and Molecular Biology, Temple University School of Medicine, 3307 North Broad Street, Philadelphia, PA 19140-5101, United States.
authors.forename: M V Ramana
authors.initials: MVR
authors.lastname: Reddy
authors.affiliation: Fels Institute for Cancer Research and Molecular Biology, Temple University School of Medicine, 3307 North Broad Street, Philadelphia, PA 19140-5101, United States.
authors.forename: Venkat R
authors.initials: VR
authors.lastname: Pallela
authors.affiliation: Fels Institute for Cancer Research and Molecular Biology, Temple University School of Medicine, 3307 North Broad Street, Philadelphia, PA 19140-5101, United States.
authors.forename: Stephen C
authors.initials: SC
authors.lastname: Cosenza
authors.affiliation: Onconova Therapeutics Inc., 375 Pheasant Run, Newtown, PA 18940, United States.
authors.forename: Muralidhar R
authors.initials: MR
authors.lastname: Mallireddigari
authors.affiliation: Onconova Therapeutics Inc., 375 Pheasant Run, Newtown, PA 18940, United States.
authors.forename: Revathi
authors.initials: R
authors.lastname: Patti
authors.affiliation: Fels Institute for Cancer Research and Molecular Biology, Temple University School of Medicine, 3307 North Broad Street, Philadelphia, PA 19140-5101, United States.
authors.forename: Marie
authors.initials: M
authors.lastname: Bonagura
authors.affiliation: Fels Institute for Cancer Research and Molecular Biology, Temple University School of Medicine, 3307 North Broad Street, Philadelphia, PA 19140-5101, United States.
authors.forename: May
authors.initials: M
authors.lastname: Truongcao
authors.affiliation: Onconova Therapeutics Inc., 375 Pheasant Run, Newtown, PA 18940, United States.
authors.forename: Balaiah
authors.initials: B
authors.lastname: Akula
authors.affiliation: Fels Institute for Cancer Research and Molecular Biology, Temple University School of Medicine, 3307 North Broad Street, Philadelphia, PA 19140-5101, United States.
authors.forename: Shashidhar S
authors.initials: SS
authors.lastname: Jatiani
authors.affiliation: Fels Institute for Cancer Research and Molecular Biology, Temple University School of Medicine, 3307 North Broad Street, Philadelphia, PA 19140-5101, United States.
authors.forename: E Premkumar
authors.initials: EP
authors.lastname: Reddy
mesh_terms: D049109:Cell Proliferation / Q000187:drug effects; D047188:Chalcones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D016044:Fusion Proteins, bcr-abl / Q000037:antagonists & inhibitors* / Q000378:metabolism; D006801:Humans; D020014:K562 Cells; D015394:Molecular Structure; D010766:Phosphorylation; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
chemical_list: C549755:(E)-alpha-benzylthio chalcone; D047188:Chalcones; D047428:Protein Kinase Inhibitors; D011505:Protein-Tyrosine Kinases; D016044:Fusion Proteins, bcr-abl