title: Total synthesis of a library of designed hybrids of the microtubule-stabilising anticancer agents taxol, discodermolide and dictyostatin.
abstract: A hybrid library of the marine natural products dictyostatin and discodermolide, incorporating the taxol or taxotere side chains, were synthesised; preliminary biological evaluation in the PANC-1 cancer cell line revealed significant antiproliferative activity, demonstrating that a macrolide scaffold is an effective surrogate for the baccatin core of taxol.
authors.affiliation: University Chemical Laboratory, Lensfield Road, Cambridge, UK, CB2 1EW. ip100@cam.ac.uk
authors.forename: Ian
authors.initials: I
authors.lastname: Paterson
authors.forename: Guy J
authors.initials: GJ
authors.lastname: Naylor
authors.forename: Takeshi
authors.initials: T
authors.lastname: Fujita
authors.forename: Esther
authors.initials: E
authors.lastname: Guzmán
authors.forename: Amy E
authors.initials: AE
authors.lastname: Wright
mesh_terms: D000473:Alkanes / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D002219:Carbamates / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D045744:Cell Line, Tumor; D006801:Humans; D007783:Lactones / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D018942:Macrolides / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D008870:Microtubules / Q000737:chemistry / Q000378:metabolism; D017239:Paclitaxel / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D011753:Pyrones / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D050257:Tubulin Modulators / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity
chemical_list: D000473:Alkanes; D000970:Antineoplastic Agents; D002219:Carbamates; D007783:Lactones; D018942:Macrolides; D011753:Pyrones; D050257:Tubulin Modulators; C470814:dictyostatin; C071229:discodermolide; D017239:Paclitaxel