Advance of Seriniquinone Analogues as Melanoma Agents.
ACS Med Chem Lett
; 10(2): 186-190, 2019 Feb 14.
Article
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| MEDLINE
| ID: mdl-30783501
ABSTRACT
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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MEDLINE
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En
Revista:
ACS Med Chem Lett
Año:
2019
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Article
País de afiliación:
Estados Unidos