title: Structure-activity & structure-toxicity relationship study of salinomycin diastereoisomers and their benzoylated derivatives.
abstract: Salinomycin diastereoisomers and their benzoylated derivatives were synthesized and evaluated for both antiproliferative activity and neurotoxicity in vitro. The results indicated that the stereoscopic configurations of the spiro C17 and C21 atoms as well as the benzoyl groups of O-20 on the rigid B/C/D spiro-ketal structures are crucial for biological activity and neural toxicity. In general, there are some positive correlations between the antiproliferative activity and neurotoxicity in these salinomycin derivatives, indicating possibly similar mechanisms of action.
authors.affiliation: State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing 100050, China. ws@imm.ac.cn.
authors.forename: Wenxuan
authors.initials: W
authors.lastname: Zhang
authors.affiliation: State Key Laboratory of Reproductive Biology, Institute of Zoology, Chinese Academy of Sciences, Beijing 100101, China. zhouqi@ioz.ac.cn.
authors.forename: Jun
authors.initials: J
authors.lastname: Wu
authors.affiliation: State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing 100050, China. ws@imm.ac.cn.
authors.forename: Bo
authors.initials: B
authors.lastname: Li
authors.affiliation: State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing 100050, China. ws@imm.ac.cn.
authors.forename: Hongna
authors.initials: H
authors.lastname: Wu
authors.affiliation: State Key Laboratory of Reproductive Biology, Institute of Zoology, Chinese Academy of Sciences, Beijing 100101, China. zhouqi@ioz.ac.cn.
authors.forename: Liu
authors.initials: L
authors.lastname: Wang
authors.affiliation: State Key Laboratory of Reproductive Biology, Institute of Zoology, Chinese Academy of Sciences, Beijing 100101, China. zhouqi@ioz.ac.cn.
authors.forename: Jie
authors.initials: J
authors.lastname: Hao
authors.affiliation: State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing 100050, China. ws@imm.ac.cn.
authors.forename: Song
authors.initials: S
authors.lastname: Wu
authors.affiliation: State Key Laboratory of Reproductive Biology, Institute of Zoology, Chinese Academy of Sciences, Beijing 100101, China. zhouqi@ioz.ac.cn.
authors.forename: Qi
authors.initials: Q
authors.lastname: Zhou
mesh_terms: D019817:Benzoic Acid / Q000737:chemistry*; D018360:Crystallography, X-Ray; D009682:Magnetic Resonance Spectroscopy; D011714:Pyrans / Q000737:chemistry* / Q000494:pharmacology*; D017550:Spectroscopy, Fourier Transform Infrared; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D000095662:Polyether Polyketides
chemical_list: D019817:Benzoic Acid; D011714:Pyrans; C010327:salinomycin; D000095662:Polyether Polyketides