title: Design, synthesis, and biological evaluation of novel 4-hydro-quinoline-3-carboxamide derivatives as an immunomodulator.
abstract: A series of novel quinoline-3-carboxamide derivatives were synthesized and evaluated for their immunomodulatory activity. The compounds were tested in vitro for effects on spleen lymphocyte proliferation and TNF-alpha production by macrophage. Three compounds showed immunomodulatory profiles similar to and more potent than those of linomide and FR137316 and were selected for further pharmacological studies in vivo.
authors.affiliation: Beijing Institute of Pharmacology and Toxicology, Department of Medicinal Chemistry, 27 Taiping Road, Beijing 100850, China. hjf3770@yahoo.com
authors.forename: Jun-Feng
authors.initials: JF
authors.lastname: He
authors.forename: Liu-Hong
authors.initials: LH
authors.lastname: Yun
authors.forename: Ri-Fang
authors.initials: RF
authors.lastname: Yang
authors.forename: Zhi-Yong
authors.initials: ZY
authors.lastname: Xiao
authors.forename: Jun-Ping
authors.initials: JP
authors.lastname: Cheng
authors.forename: Wen-Xia
authors.initials: WX
authors.lastname: Zhou
authors.forename: Yong-Xiang
authors.initials: YX
authors.lastname: Zhang
mesh_terms: D000818:Animals; D049109:Cell Proliferation / Q000187:drug effects*; D002478:Cells, Cultured; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D006912:Hydroxyquinolines / Q000494:pharmacology; D007155:Immunologic Factors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D008214:Lymphocytes / Q000187:drug effects / Q000276:immunology; D008264:Macrophages / Q000187:drug effects / Q000276:immunology / Q000378:metabolism*; D011804:Quinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D013154:Spleen / Q000187:drug effects / Q000276:immunology; D014409:Tumor Necrosis Factor-alpha / Q000378:metabolism
chemical_list: D006912:Hydroxyquinolines; D007155:Immunologic Factors; D011804:Quinolines; D014409:Tumor Necrosis Factor-alpha; C045282:roquinimex