title: Synthesis and in vitro evaluation of 4-substituted furano[3,2-c] tetrahydroquinolines as potential anti-cancer agents.
abstract: A convenient and mild method for the synthesis of substituted furano [3,2-c]tetrahydroquinoline derivatives was developed, using the multi-component Povarov reaction. Of the synthesized tetrahydroquinoline derivatives, compound 10a displayed the greatest cellular proliferation inhibitory activities with IC50 values of 2.5-16.7 μmol/l. In addition, 10a induced murine C6 glioma cell apoptosis in a dose-dependent manner by up-regulating the expression of Bax, caspase-3, and caspase-9, and by down-regulating Bcl-2. Our findings suggest that these novel compounds have potential as therapeutic agents via inducing mitochondrial apoptosis.
authors.affiliation: a College of Pharmacy and the First Affiliated Hospital, Chengdu Medical College , Chengdu , PR China .|b Department of Pharmacy , Sichuan Provincial People's Hospital , Chengdu , PR China .
authors.forename: Can
authors.initials: C
authors.lastname: Chen
authors.affiliation: c Department of Chemistry , Armstrong State University , Savannah , GA , USA , and.
authors.forename: Sarah
authors.initials: S
authors.lastname: Zingales
authors.affiliation: d Department of Cardiology , General Hospital of Chengdu Military Command , Chengdu , PR China.
authors.forename: Ting
authors.initials: T
authors.lastname: Wang
authors.affiliation: a College of Pharmacy and the First Affiliated Hospital, Chengdu Medical College , Chengdu , PR China .
authors.forename: Mingyong
authors.initials: M
authors.lastname: Yuan
authors.affiliation: a College of Pharmacy and the First Affiliated Hospital, Chengdu Medical College , Chengdu , PR China .
authors.forename: Dan
authors.initials: D
authors.lastname: Wang
authors.affiliation: b Department of Pharmacy , Sichuan Provincial People's Hospital , Chengdu , PR China .
authors.forename: Lulu
authors.initials: L
authors.lastname: Cai
authors.affiliation: a College of Pharmacy and the First Affiliated Hospital, Chengdu Medical College , Chengdu , PR China .|d Department of Cardiology , General Hospital of Chengdu Military Command , Chengdu , PR China.
authors.forename: Qinglin
authors.initials: Q
authors.lastname: Jiang
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects*; D045744:Cell Line, Tumor; D005663:Furans / Q000138:chemical synthesis* / Q000494:pharmacology*; D015972:Gene Expression Regulation, Neoplastic / Q000187:drug effects; D051379:Mice; D008928:Mitochondria / Q000187:drug effects; D015394:Molecular Structure; D011804:Quinolines / Q000138:chemical synthesis* / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D005663:Furans; D011804:Quinolines; C542964:1,2,3,4-tetrahydroquinoline
keywords: Antitumor activity; apoptosis; diastereoselectivity; tetrahydroquinoline derivatives