title: Synthesis and cytotoxicity of thieno[2,3-b]quinoline-2-carboxamide and cycloalkyl[b]thieno[3,2-e]pyridine-2-carboxamide derivatives.
abstract: Seventy nine derivatives of thieno[2,3-b]quinolines, tetrahydrothieno[2,3-b]quinoline, dihydrocyclopenta[b]thieno[3,2-e]pyridine, cyclohepta[b]thieno[3,2-e]pyridine and hexahydrocycloocta[b]thieno[3,2-e]pyridine were either synthesized or obtained commercially and tested for their antiproliferative activity against HCT116, MDA-MB-468 and MDA-MB-231 human cancer cell lines. The most potent eight compounds were active against all cell lines with IC50 values in the 80-250nM range. In general hexahydrocycloocta[b]thieno[3,2-e]pyridines were most active with increasing activity observed as larger cycloalkyl rings were fused to the pyridine ring.
authors: Auckland Cancer Society Research Centre, The University of Auckland, New Zealand; Department of Molecular Medicine and Pathology, The University of Auckland, New Zealand. Electronic address: e.leung@auckland.ac.nz.
authors: Euphemia
authors: E
authors: Leung
authors: Auckland Cancer Society Research Centre, The University of Auckland, New Zealand; School of Chemical Sciences, The University of Auckland, New Zealand.
authors: Lisa I
authors: LI
authors: Pilkington
authors: School of Chemical Sciences, The University of Auckland, New Zealand.
authors: Michelle
authors: M
authors: van Rensburg
authors: School of Chemical Sciences, The University of Auckland, New Zealand.
authors: Chae Yeon
authors: CY
authors: Jeon
authors: School of Chemical Sciences, The University of Auckland, New Zealand.
authors: Mirae
authors: M
authors: Song
authors: School of Chemical Sciences, The University of Auckland, New Zealand.
authors: Homayon J
authors: HJ
authors: Arabshahi
authors: School of Chemical Sciences, The University of Auckland, New Zealand.
authors: Gayan Heruka
authors: GH
authors: De Zoysa
authors: School of Chemical Sciences, The University of Auckland, New Zealand.
authors: Vijayalekshmi
authors: V
authors: Sarojini
authors: Auckland Cancer Society Research Centre, The University of Auckland, New Zealand.
authors: William A
authors: WA
authors: Denny
authors: School of Chemical Sciences, The University of Auckland, New Zealand. Electronic address: j.reynisson@auckland.ac.nz.
authors: Jóhannes
authors: J
authors: Reynisson
authors: School of Chemical Sciences, The University of Auckland, New Zealand. Electronic address: d.barker@auckland.ac.nz.
authors: David
authors: D
authors: Barker
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy; D011804:Quinolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D058924:Thienopyridines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D011804:Quinolines; D058924:Thienopyridines; C541322:quinoline-3-carboxamide
keywords: Antiproliferative; Thieno[2,3-b]pyridines; Thieno[2,3-b]quinolones; Thieno[3,2-e]pyridines