title: Preparation of leukotriene B(4) inhibitory active 2- and 3-(2-aminothiazol-4-yl)benzo[b]furan derivatives and their growth inhibitory activity on human pancreatic cancer cells.
abstract: A series of 2-(2-aminothiazol-4-yl)benzo[b]furan and 3-(2-aminothiazol-4-yl)benzo[b]furan derivatives were prepared, and their leukotriene B(4) inhibitory activity and growth inhibitory activity in cancer cell lines were evaluated. Several compounds showed strong inhibition of calcium mobilization in CHO cells overexpressing human BLT(1) and BLT(2) receptors and growth inhibition to human pancreatic cancer cells MIA PaCa-2. 3-(4-Chlorophenyl)-2-[5-formyl-2-[(dimethylamino)methyleneamino]thiazol-4-yl]-5-methoxybenzo[b]furan 8b showed the most potent and selective inhibition for the human BLT(2) receptor, and its IC(50) value was smaller than that of the selected positive control compound, ZK-158252. 3-(4-Chlorophenyl)-2-[2-[(dimethylamino)methyleneamino]-5-(2-hydroxyethyliminomethyl)thiazol-4-yl]-5-methoxybenzo[b]furan 9a displayed growth inhibitory activity towards MIA PaCa-2.
authors.affiliation: School of Pharmaceutical Sciences, Mukogawa Women's University, Nishinomiya, Japan.
authors.forename: Mari
authors.initials: M
authors.lastname: Kuramoto
authors.forename: Yoko
authors.initials: Y
authors.lastname: Sakata
authors.forename: Kumi
authors.initials: K
authors.lastname: Terai
authors.forename: Ikuo
authors.initials: I
authors.lastname: Kawasaki
authors.forename: Jun-Ichi
authors.initials: J
authors.lastname: Kunitomo
authors.forename: Takahiro
authors.initials: T
authors.lastname: Ohishi
authors.forename: Takehiko
authors.initials: T
authors.lastname: Yokomizo
authors.forename: Seiichi
authors.initials: S
authors.lastname: Takeda
authors.forename: Shuichi
authors.initials: S
authors.lastname: Tanaka
authors.forename: Yoshitaka
authors.initials: Y
authors.lastname: Ohishi
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000627:therapeutic use; D001572:Benzofurans / Q000737:chemistry* / Q000627:therapeutic use; D016466:CHO Cells; D045744:Cell Line, Tumor; D006224:Cricetinae; D003412:Cricetulus; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D010190:Pancreatic Neoplasms / Q000188:drug therapy*; D018102:Receptors, Leukotriene B4 / Q000037:antagonists & inhibitors* / Q000187:drug effects; D013844:Thiazoles / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D001572:Benzofurans; D018102:Receptors, Leukotriene B4; D013844:Thiazoles; C004483:2-aminothiazole