title: Synthesis and anti-cancer activities of apigenin derivatives.
abstract: A novel series of apigenin derivatives with phloroglucinol or resorcinol as raw materials were synthesized according to Baker-Venaktaraman reaction and their in vitro inhibitory activities on colorectal adenocarcinoma (HT-29) and leucocythemia (HL-60) cell lines were evaluated by the standard methyl thiazole tetrazolium (MTT) method. The results of biological test showed that some of apigenin derivatives possessed stronger anti-cancer activities than apigenin. Compound 6 showed the strongest activity against colorectal adenocarcinoma (HT-29) and leucocythemia (HL-60) cell lines with IC50 valure of 2.03±0.22 µM, 2.25±0.42 µM, it was better than 5-FU (12.92±0.61 µM, 9.56±0.16 µM), which shows a potential compound for colorectal adenocarcinoma and leucocythemia.
authors.forename: Xing
authors.initials: X
authors.lastname: Zheng
authors.forename: Liuying
authors.initials: L
authors.lastname: Yu
authors.forename: Jing
authors.initials: J
authors.lastname: Yang
authors.forename: Xu
authors.initials: X
authors.lastname: Yao
authors.forename: Wenna
authors.initials: W
authors.lastname: Yan
authors.forename: Shaowei
authors.initials: S
authors.lastname: Bo
authors.forename: Ya
authors.initials: Y
authors.lastname: Liu
authors.forename: Yun
authors.initials: Y
authors.lastname: Wei
authors.forename: Zhiyi
authors.initials: Z
authors.lastname: Wu
authors.affiliation: Institute of Pharmacy & Pharmacology, University of South China, Hengyang, 421001, China. zhengxing5018@yahoo.com.
authors.forename: Guan
authors.initials: G
authors.lastname: Wang
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D047310:Apigenin / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D016923:Cell Death / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D018922:HL-60 Cells; D019073:HT29 Cells; D006801:Humans; D015394:Molecular Structure; D008970:Molecular Weight; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D047310:Apigenin