title: Design, synthesis, and anti-tumor activities of novel triphenylethylene-coumarin hybrids, and their interactions with Ct-DNA.
abstract: Novel triphenylethylene-coumarin hybrid derivatives containing different amounts of amino side chains were designed and synthesized in good yields under microwave radiation. The derivatives 5b-d which possessed two amino side chains (except morpholinyl) showed a broad-spectrum and good anti-proliferative activity against five tumor cells and low cytotoxicity in osteoblast. UV-vis, fluorescence, and circular dichroism (CD) spectroscopies and thermal denaturation exhibited that compounds 10 c, 5c, and 13c bearing amino side chain (except morpholinyl) on 4-phenyl had significant interactions with Ct-DNA by the intercalative mode of binding. Structure-activity relationships (SARs) analysis suggested that the amino alkyl chain would play an important role both in the compounds against tumor cells proliferation and their interactions with DNA.
authors.affiliation: Key Laboratory of Chemical Biology of Hebei Province, College of Chemistry and Environmental Science, Hebei University, Baoding 071002, China.
authors.forename: Hua
authors.initials: H
authors.lastname: Chen
authors.forename: Shuai
authors.initials: S
authors.lastname: Li
authors.forename: Yuchao
authors.initials: Y
authors.lastname: Yao
authors.forename: Likai
authors.initials: L
authors.lastname: Zhou
authors.forename: Jianpeng
authors.initials: J
authors.lastname: Zhao
authors.forename: Yunjing
authors.initials: Y
authors.lastname: Gu
authors.forename: Kerang
authors.initials: K
authors.lastname: Wang
authors.forename: Xiaoliu
authors.initials: X
authors.lastname: Li
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D002417:Cattle; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D003374:Coumarins / Q000737:chemistry* / Q000494:pharmacology*; D004247:DNA / Q000378:metabolism*; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D007364:Intercalating Agents / Q000737:chemistry / Q000494:pharmacology; D009369:Neoplasms / Q000188:drug therapy; D013267:Stilbenes / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D003374:Coumarins; D007364:Intercalating Agents; D013267:Stilbenes; D004247:DNA; C427203:calf thymus DNA; C030123:coumarin; C037749:triphenylethylene
keywords: Anti-tumor activities; Coumarin; DNA binding property; Triphenylethylene