期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 10, 期 2, 页码 186-190出版社
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.8b00391
关键词
Drug discovery; melanoma; marine natural products; medicinal chemistry; seriniquinone; dermcidin
资金
- NIH, National Cancer Institute [CA 044848]
- Taubman Foundation
- FAPESP [2015/17117-6, 2016/10854-5, 2018/07661-6]
- Fundacao de Amparo a Pesquisa do Estado de Sao Paulo (FAPESP) [18/07661-6] Funding Source: FAPESP
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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