title: Synthesis and evaluation of double bond substituted combretastatins.
abstract: A series of combretastatins substituted with epoxides, amides and small alkyl groups has been synthesised and evaluated for cytotoxicity and their ability to inhibit the assembly of tubulin. The methyl and ethyl substituted phenols 36, 44 have shown potent antimitotic effects whilst exhibiting reduced cytotoxicity.
authors.affiliation: Centre for Molecular Drug Design, Cockcroft Building, University of Salford, Manchester M5 4WT, UK. j.a.hadfield@salford.ac.uk
authors.forename: John A
authors.initials: JA
authors.lastname: Hadfield
authors.forename: Keira
authors.initials: K
authors.lastname: Gaukroger
authors.forename: Nicholas
authors.initials: N
authors.lastname: Hirst
authors.forename: Anna P
authors.initials: AP
authors.lastname: Weston
authors.forename: Nicholas J
authors.initials: NJ
authors.lastname: Lawrence
authors.forename: Alan T
authors.initials: AT
authors.lastname: McGown
mesh_terms: D000577:Amides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001632:Bibenzyls / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002453:Cell Cycle / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D004852:Epoxy Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D005562:Formazans / Q000737:chemistry; D006801:Humans; D020128:Inhibitory Concentration 50; D020014:K562 Cells; D009682:Magnetic Resonance Spectroscopy; D015394:Molecular Structure; D013056:Spectrophotometry, Ultraviolet; D013267:Stilbenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013778:Tetrazolium Salts / Q000737:chemistry; D014404:Tubulin / Q000378:metabolism; D050257:Tubulin Modulators
chemical_list: D000577:Amides; D000970:Antineoplastic Agents; D001632:Bibenzyls; D004852:Epoxy Compounds; D005562:Formazans; D013267:Stilbenes; D013778:Tetrazolium Salts; D014404:Tubulin; D050257:Tubulin Modulators; C079782:MTT formazan; C040105:combretastatin