Ontology highlight
ABSTRACT:
SUBMITTER: Morgan JB
PROVIDER: S-EPMC2918693 | biostudies-literature | 2010 Aug
REPOSITORIES: biostudies-literature
Morgan J Brian JB Mahdi Fakhri F Liu Yang Y Coothankandaswamy Veena V Jekabsons Mika B MB Johnson Tyler A TA Sashidhara Koneni V KV Crews Phillip P Nagle Dale G DG Zhou Yu-Dong YD
Bioorganic & medicinal chemistry 20100625 16
A natural product chemistry-based approach was applied to discover small-molecule inhibitors of hypoxia-inducible factor-1 (HIF-1). A Petrosaspongia mycofijiensis marine sponge extract yielded mycothiazole (1), a solid tumor selective compound with no known mechanism for its cell line-dependent cytotoxic activity. Compound 1 inhibited hypoxic HIF-1 signaling in tumor cells (IC(50) 1nM) that correlated with the suppression of hypoxia-stimulated tumor angiogenesis in vitro. However, 1 exhibited pr ...[more]