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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

Advance of Seriniquinone Analogues as Melanoma Agents

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Hammons, Justin C. [1] ; Trzoss, Lynnie [1] ; Jimenez, Paula C. [2] ; Hirata, Amanda S. [3] ; Costa-Lotufo, Leticia V. [3] ; La Clair, James J. [4] ; Fenical, William [1]
Total Authors: 7
[1] Univ Calif San Diego, Scripps Inst Oceanog, Ctr Marine Biotechnol & Biomed, La Jolla, CA 92093 - USA
[2] Univ Fed Sao Paulo, Inst Mar, BR-11070100 Santos, SP - Brazil
[3] Univ Sao Paulo, Inst Ciencias Biomed, BR-05508900 Sao Paulo, SP - Brazil
[4] Univ Calif San Diego, Dept Chem & Biochem, 9500 Gilman Dr, La Jolla, CA 92093 - USA
Total Affiliations: 4
Document type: Journal article
Source: ACS Medicinal Chemistry Letters; v. 10, n. 2, p. 186-190, FEB 2019.
Web of Science Citations: 0

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. (AU)

FAPESP's process: 16/10854-5 - Investigation of cytotoxic mechanisms of synthetic derivatives of seriniquinone in melanoma cell lines
Grantee:Amanda Soares Hirata
Support type: Scholarships in Brazil - Scientific Initiation
FAPESP's process: 18/07661-6 - Seriniquinone and its derivative LT406 as antimelanoma agents in experimental models
Grantee:Amanda Soares Hirata
Support type: Scholarships in Brazil - Master