Synthesis and antiproliferative activity of C- and N-terminal analogues of culicinin D

[Display omitted] Culicinin D (1), a 10 amino acid peptaibol containing several unusual residues, has been shown to exhibit potent anticancer activity. Previous work in our group towards developing a structure-activity relationship (SAR) for this peptaibol has concentrated on replacement of the synt...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2020-08, Vol.30 (16), p.127331-127331, Article 127331
Main Authors: Li, Freda F., Stubbing, Louise A., Kavianinia, Iman, Abbattista, Maria R., Harris, Paul W.R., Smaill, Jeff B., Patterson, Adam V., Brimble, Margaret A.
Format: Article
Language:English
Subjects:
Cancer
Culicinin D
Peptaibol
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Summary:[Display omitted] Culicinin D (1), a 10 amino acid peptaibol containing several unusual residues, has been shown to exhibit potent anticancer activity. Previous work in our group towards developing a structure-activity relationship (SAR) for this peptaibol has concentrated on replacement of the synthetically challenging AHMOD (3) and AMD (4) residues, resulting in the discovery of analogues with equivalent or better potency and simplified synthesis. The SAR of this peptaibol is extended in this work by investigating the effect of the N-terminal lipid tail and C-terminal amino alcohol, revealing the key contribution of each of these moieties on antiproliferative activity in a panel of breast and lung cancer cell lines.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2020.127331