title: Structure-activity relationships of diverse annonaceous acetogenins against human tumor cells.
abstract: Twelve annonaceous acetogenins (ACGs) with different stereochemical structures and configuration were selected to test for their inhibitions on the growth of Hela, SMMC-7541, SGC-7901, MCF-7 and A-5408 tumor cell lines using MTT method. This was the first to simultaneously investigate effects of structural factors of stereochemical structures and configuration on cytotoxicities with structure-activity relationship. The present study showed that cytotoxic selectivities of ACGs with threo/trans/threo/trans/erythro stereochemical arrangement were gently more active than those with threo/trans/threo/trans/threo stereochemical arrangement, and ACGs with cis THF ring partly produced notable cytotoxic selectivities. Furthermore, ACGs with S configuration at C-24 exhibited gently more cytotoxic selectivities potency than those with R configuration at C-24.
authors.affiliation: Department of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, China. yanghaijunzn@163.com
authors.forename: Haijun
authors.initials: H
authors.lastname: Yang
authors.forename: Ning
authors.initials: N
authors.lastname: Zhang
authors.forename: Xiang
authors.initials: X
authors.lastname: Li
authors.forename: Jianwei
authors.initials: J
authors.lastname: Chen
authors.forename: Baochang
authors.initials: B
authors.lastname: Cai
mesh_terms: D054378:Acetogenins / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology*; D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D006367:HeLa Cells; D006801:Humans; D010936:Plant Extracts / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
chemical_list: D054378:Acetogenins; D000972:Antineoplastic Agents, Phytogenic; D010936:Plant Extracts