title: Cytotoxic Evaluation against Breast Cancer Cells of Isoliquiritigenin Analogues from Spatholobus suberectus and Their Synthetic Derivatives.
abstract: Five isoliquiritigenin analogues, including a new methylene-bridged bischalcone (1), were isolated from Spatholobus suberectus. Cytotoxicity screening of these isolates and several synthetic derivatives indicated that the introduction, removal, position modification, or glycosylation of hydroxy groups in isoliquiritigenin did not improve the resultant cytotoxicity against the MCF-7 and MDA-MB-231 human breast cancer cell lines. In addition, cyclization of OH-2' chalcones or reduction of the α,β-unsaturated carbonyl double bond decreased such cytotoxicity substantially. However, methylation of hydroxy groups resulted in a marked increase in such cytotoxic activity. Among these active isoliquiritigenin analogues, 3',4',5',4″-tetramethoxychalcone (3h) was obtained as a compound with promising cytotoxic activity.
authors.affiliation: School of Chinese Medicine, The University of Hong Kong , 10 Sassoon Road, Pokfulam, Hong Kong, People's Republic of China.
authors.forename: Fu
authors.initials: F
authors.lastname: Peng
authors.forename: Chun-Wang
authors.initials: CW
authors.lastname: Meng
authors.forename: Qin-Mei
authors.initials: QM
authors.lastname: Zhou
authors.affiliation: School of Chinese Medicine, The University of Hong Kong , 10 Sassoon Road, Pokfulam, Hong Kong, People's Republic of China.
authors.forename: Jian-Ping
authors.initials: JP
authors.lastname: Chen
authors.forename: Liang
authors.initials: L
authors.lastname: Xiong
mesh_terms: D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D001943:Breast Neoplasms / Q000188:drug therapy; D049109:Cell Proliferation / Q000187:drug effects; D047188:Chalcones / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D004354:Drug Screening Assays, Antitumor; D004365:Drugs, Chinese Herbal / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D007887:Fabaceae / Q000737:chemistry*; D005260:Female; D006801:Humans; D015394:Molecular Structure
chemical_list: C000608590:3',4',5',4''-tetramethoxychalcone; D000972:Antineoplastic Agents, Phytogenic; D047188:Chalcones; D004365:Drugs, Chinese Herbal; C000608589:methylenebisisoliquiritigenin; C040920:isoliquiritigenin