title: Synthesis of new thieno[2,3-b]pyridine derivatives as pim-1 inhibitors.
abstract: Three series of 5-bromo-thieno[2,3-b]pyridines bearing amide or benzoyl groups at position 2 were prepared as pim-1 inhibitors. All the prepared compounds were tested for their pim-1 enzyme inhibitory activity. Two compounds (3c and 5b) showed moderate pim-1 inhibitory activity with IC50 of 35.7 and 12.71 μM, respectively. Three other compounds (3d, 3g and 6d) showed poor pim-1 inhibition. The most active compounds were tested for their cytotoxic activity on five cell lines [MCF7, HEPG2, HCT116, A549 and PC3]. Compound 3g was the most potent cytotoxic agent on almost all the cell lines tested.
authors.affiliation: a Pharmaceutical Chemistry Department , Faculty of Pharmacy, The British University in Egypt , Cairo , Egypt and.|b Pharmaceutical Organic Chemistry Department , Faculty of Pharmacy, Cairo University , Cairo , Egypt.
authors.forename: Bassem H
authors.initials: BH
authors.lastname: Naguib
authors.affiliation: b Pharmaceutical Organic Chemistry Department , Faculty of Pharmacy, Cairo University , Cairo , Egypt.
authors.forename: Hala B
authors.initials: HB
authors.lastname: El-Nassan
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D051573:Proto-Oncogene Proteins c-pim-1 / Q000037:antagonists & inhibitors*; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D047428:Protein Kinase Inhibitors; D011725:Pyridines; D051573:Proto-Oncogene Proteins c-pim-1
keywords: Cytotoxic activity; pim-1; thieno[2,3-b]pyridine