Synthesis and biological evaluation of novel analogues of dictyostatin.
Novel analogues of the microtubule-stabilising agent dictyostatin were designed using existing SAR information from the structurally related discodermolide, synthesised by a late-stage diversification strategy and evaluated in vitro for growth inhibition against a range of human cancer cell lines, including those known to exhibit Taxol-resistance (AsPC-1, DLD-1, PANC-1, NCI/ADR).
Paterson
Ian
I
University Chemical Laboratory, Lensfield Road, Cambridge CB2 1EW, UK. ip100@cam.ac.uk
Gardner
Nicola M
NM
Poullennec
Karine G
KG
Wright
Amy E
AE
D000972:Antineoplastic Agents, Phytogenic; D045744:Cell Line, Tumor; D002626:Chemistry, Pharmaceutical / Q000379:methods; D015195:Drug Design; D019008:Drug Resistance, Neoplasm; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D018942:Macrolides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D008956:Models, Chemical; D008968:Molecular Conformation; D017239:Paclitaxel / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000972:Antineoplastic Agents, Phytogenic; D018942:Macrolides; C470814:dictyostatin; D017239:Paclitaxel