Hammons, Justin C.
Jimenez, Paula C.
Hirata, Amanda S.
Costa-Lotufo, Leticia V.
La Clair, James J.
Total Authors: 7
 Univ Calif San Diego, Scripps Inst Oceanog, Ctr Marine Biotechnol & Biomed, La Jolla, CA 92093 - USA
 Univ Fed Sao Paulo, Inst Mar, BR-11070100 Santos, SP - Brazil
 Univ Sao Paulo, Inst Ciencias Biomed, BR-05508900 Sao Paulo, SP - Brazil
 Univ Calif San Diego, Dept Chem & Biochem, 9500 Gilman Dr, La Jolla, CA 92093 - USA
Total Affiliations: 4
ACS Medicinal Chemistry Letters;
Web of Science Citations:
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)