title: Synthesis, cytotoxicities and DNA-binding affinities of benzofuran-3-ols and their fused analogs.
abstract: A series of benzofuropyrazoles 2a-i were synthesized in 10-92% from the reaction of 2-aroylbenzofuran-3-ols 1a-i with hydrazine hydrate, and screened for their antitumor activities toward four human solid tumor cell lines, including gastric carcinoma cells MKN45, hepatocellular carcinoma cells HepG2, breast cancer cells MCF-7, and lung cancer cells A549. The results indicated that both compounds 1a-i and 2a-i displayed moderate antitumor activities. Among them, compound 2e exhibited potent inhibitory activity toward all the four tumor cell lines. In addition, compounds 1e and 2e showed strong DNA-binding affinities, and induced an increase in the viscosity of calf-thymus DNA, suggesting that they might act as an intercalator.
authors.affiliation: School of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, China.
authors.forename: Zhong-Zhen
authors.initials: ZZ
authors.lastname: Zhou
authors.forename: Min
authors.initials: M
authors.lastname: Zou
authors.forename: Jia
authors.initials: J
authors.lastname: Zhou
authors.forename: Chun-Qiong
authors.initials: CQ
authors.lastname: Zhou
authors.forename: Yan-Hong
authors.initials: YH
authors.lastname: Deng
authors.forename: Ming-Hui
authors.initials: MH
authors.lastname: Chen
authors.forename: Chun-Ping
authors.initials: CP
authors.lastname: Gu
authors.forename: Zhi-Hong
authors.initials: ZH
authors.lastname: Jiang
authors.forename: Wen-Hua
authors.initials: WH
authors.lastname: Chen
authors.forename: Shu-Wen
authors.initials: SW
authors.lastname: Liu
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D001572:Benzofurans / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D002417:Cattle; D045744:Cell Line, Tumor; D004247:DNA / Q000378:metabolism; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy*; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D001572:Benzofurans; D011720:Pyrazoles; D004247:DNA; C427203:calf thymus DNA