Design, synthesis and biological evaluation of novel, simplified analogues of laulimalide: modification of the side chain.
Novel, simplified analogues of the microtubule-stabilizing anticancer agent laulimalide, including the first derivatives with unnatural side chains, were designed by molecular modelling, synthesized by a late-stage diversification strategy, and evaluated in vitro for growth inhibition of human ovarian carcinoma cell lines (A2780, A2780/AD10).
Paterson
Ian
I
University Chemical Laboratory, Lensfield Road, Cambridge CB2 1EW, UK, EU. ip100@cam.ac.uk
Menche
Dirk
D
Håkansson
Anders E
AE
Longstaff
Adrian
A
Wong
David
D
Barasoain
Isabel
I
Buey
Rubén M
RM
Díaz
J Fernando
JF
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002455:Cell Division / Q000187:drug effects*; D045744:Cell Line, Tumor; D015195:Drug Design; D005260:Female; D006801:Humans; D018942:Macrolides; D008958:Models, Molecular; D008968:Molecular Conformation; D015394:Molecular Structure; D010051:Ovarian Neoplasms; D013329:Structure-Activity Relationship; D043823:Taxoids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
D000970:Antineoplastic Agents; D018942:Macrolides; D043823:Taxoids; C117305:laulimalide