title: Potent antitumor mimetics of annonaceous acetogenins embedded with an aromatic moiety in the left hydrocarbon chain part.
abstract: Annonaceous acetogenins are a large family of naturally occurring polyketides exhibiting remarkable anticancer activities. The first generation of annonaceous acetogenin mimetic (1, AA005) exhibits comparable activity as that of natural products and presents much higher selectivity between cancer and normal cells. In this work, we report the design, synthesis, and evaluation of a new series of compound 1 analogues in which a variety of conformation-constrained fragments were embedded in the left hydrocarbon chain part. Compound 7 bearing a biphenyl moiety was identified to exhibit more potent antiproliferative activity and preferentially target cancer cells over normal cells and thus represents a new lead for further optimization.
authors.affiliation: Laboratory of Regenerative Biology, Guangzhou Institute of Biomedicine and Health, Chinese Academy of Sciences, Guangzhou 510530, China.
authors.forename: Qicai
authors.initials: Q
authors.lastname: Xiao
authors.forename: Yongqiang
authors.initials: Y
authors.lastname: Liu
authors.forename: Yatao
authors.initials: Y
authors.lastname: Qiu
authors.forename: Guangbiao
authors.initials: G
authors.lastname: Zhou
authors.forename: Chan
authors.initials: C
authors.lastname: Mao
authors.forename: Zheng
authors.initials: Z
authors.lastname: Li
authors.forename: Zhu-Jun
authors.initials: ZJ
authors.lastname: Yao
authors.forename: Sheng
authors.initials: S
authors.lastname: Jiang
mesh_terms: D054378:Acetogenins / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D008968:Molecular Conformation; D018716:Molecular Mimicry; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D054378:Acetogenins; D000970:Antineoplastic Agents