title: Synthesis and antiproliferative activities of N-(naphthalen-2-yl)acetamide and N-(substituted phenyl)acetamide bearing quinolin-2(1H)-one and 3,4-dihydroquinolin-2(1H)-one derivatives.
abstract: Certain N-(naphthalen-2-yl)acetamide and N-(substituted phenyl)acetamide bearing quinolin-2(1H)-one and 3,4-dihydroquinolin-2(1H)-one derivatives have been synthesized and evaluated in vitro for their antiproliferative activities against a panel of human cancer cell lines including nasopharyngeal (NPC-TW01), lung carcinoma (H661), hepatoma (Hep3B), renal carcinoma (A498), and gastric cancer (MKN45). Among them, N-(naphthalen-2-yl)-2-(2-oxo-1,2,3,4-tetrahydroquinolin-6-yloxy)acetamide (18) was the most active against NPC-TW01 with an IC(50) value of 0.6 μM. Studies on NPC-TW01 cell cycle distribution revealed that compound 18 inhibited proliferation of NPC-TW01 by the alteration of cell division, accumulation of cells in S phase in a time- and concentration-dependent manners. In addition, compound 18 demonstrated very specific cytotoxicity against human nasopharyngeal carcinoma (NPC-TW01) cell lines with no detectable cytotoxicity against peripheral blood mononuclear cells (PBMCs) at a concentration of up to 50 μM.
authors.affiliation: Department of Pharmacy, Tajen University, Pingtung, Taiwan.
authors.forename: I-Li
authors.initials: IL
authors.lastname: Chen
authors.forename: Jih-Jung
authors.initials: JJ
authors.lastname: Chen
authors.forename: Yu-Chin
authors.initials: YC
authors.lastname: Lin
authors.forename: Ching-Tien
authors.initials: CT
authors.lastname: Peng
authors.forename: Shin-Hun
authors.initials: SH
authors.lastname: Juang
authors.forename: Tai-Chi
authors.initials: TC
authors.lastname: Wang
mesh_terms: D000081:Acetamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D006801:Humans; D007963:Leukocytes, Mononuclear / Q000187:drug effects; D015394:Molecular Structure; D009281:Naphthalenes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D015363:Quinolones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D016196:S Phase / Q000187:drug effects
chemical_list: D000081:Acetamides; D000970:Antineoplastic Agents; D009281:Naphthalenes; D015363:Quinolones; C031721:naphthalene; C030686:acetamide