title: Synthetic modification of salinomycin: selective O-acylation and biological evaluation.
abstract: Salinomycin has found renewed interest as an agent for prevention of cancer recurrence through selectively targeting cancer stem cells. Strategies for generation of improved salinomycin analogs by individual modification of its hydroxyl groups are presented. An evaluation of the dose-response effects of the resulting library on breast cancer cell lines shows that acylation of the C20 hydroxyl can be used to improve IC50 values down to one fifth that of salinomycin.
authors.affiliation: Centre for Analysis and Synthesis, Department of Chemistry, Lund University, Box 124, 221 00 Lund, Sweden. daniel.strand@chem.lu.se.
authors.forename: Björn
authors.initials: B
authors.lastname: Borgström
authors.forename: Xiaoli
authors.initials: X
authors.lastname: Huang
authors.forename: Martin
authors.initials: M
authors.lastname: Pošta
authors.forename: Cecilia
authors.initials: C
authors.lastname: Hegardt
authors.forename: Stina
authors.initials: S
authors.lastname: Oredsson
authors.forename: Daniel
authors.initials: D
authors.lastname: Strand
mesh_terms: D000215:Acylation; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology; D001943:Breast Neoplasms / Q000188:drug therapy*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D005260:Female; D006801:Humans; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D011714:Pyrans / Q000737:chemistry* / Q000494:pharmacology; D000095662:Polyether Polyketides
chemical_list: D000970:Antineoplastic Agents; D011714:Pyrans; C010327:salinomycin; D000095662:Polyether Polyketides