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Advance of seriniquinone analogues as melanoma agents

TitleAdvance of seriniquinone analogues as melanoma agents
Publication TypeJournal Article
Year of Publication2019
AuthorsHammons J.C, Trzoss L., Jimenez P.C, Hirata A.S, Costa-Lotufo L.V, La Clair J.J, Fenical W
Date Published2019/02
Type of ArticleArticle
ISBN Number1948-5875
Accession NumberWOS:000459224200006
Keywordsdermcidin; drug discovery; epigenetics; kinase; marine natural products; medicinal chemistry; melanoma; Pharmacology & Pharmacy; seriniquinone; trametinib

Seriniquinone, a marine natural product, displayed potent cytotoxicity and selectivity against melanoma cancer cells. This selectivity, combined with a novel mode of action (MOA), prompted studies to translate a pharmacologically relevant lead. Herein, we report on structure-activity relationships (SARs), and provide a strategy to prepare analogues that retain activity and offer an improved water solubility and isomeric purity. From intermediates made on a gram-scale, derivatives were prepared and evaluated for their antiproliferation activity and melanoma selectivity. Overall these studies provide methods to install side chain motifs that demonstrate a common, and yet unique, biological profile.

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