Synthesis and anticancer activity of sclerophytin-inspired hydroisobenzofurans

作者: T. David Bateman , Aarti L. Joshi , Kwangyul Moon , Elena N. Galitovskaya , Meenakshi Upreti

DOI: 10.1016/J.BMCL.2009.10.079

关键词: Bicyclic moleculeChemistryCytotoxicityEpidermoid carcinomaChemical synthesisCell growthIn vitroCell cultureStructure–activity relationshipStereochemistryOrganic chemistryClinical biochemistryMolecular medicineBiochemistryMolecular biologyDrug discoveryPharmaceutical Science

摘要: Abstract Three structurally related sets of hydroisobenzofuran analogs sclerophytin A were prepared in three or four steps from ( S )-(+)-carvone via an aldol-cycloaldol sequence. The most potent members each set exhibited IC 50 ’s 1–3 μM growth inhibitory assays against KB3 cells. NCI 60-cell line 5-dose assay for analog 6h revealed a GI  = 0.148 μM and LC  = 9.36 μM the RPMI-8226 leukemia cell line,  = 0.552 μM  = 26.8 μM HOP-92 non-small lung cancer line.

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