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Updated: Jun 18, 2026
Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Synthesis and anticancer activity of sclerophytin-inspired hydroisobenzofurans
T David Bateman1, Aarti L Joshi, Kwangyul Moon
1Department of Chemistry and Biochemistry, 119 Chemistry Building, University of Arkansas, Fayetteville, AR 72701, USA.
Abstract:
Three structurally related sets of hydroisobenzofuran analogs of sclerophytin A were prepared in three or four steps from (S)-(+)-carvone via an aldol-cycloaldol sequence. The most potent members of each set of analogs exhibited IC(50)'s of 1-3 microM in growth inhibitory assays against KB3 cells. The NCI 60-cell line 5-dose assay for analog 6h revealed a GI(50)=0.148 microM and LC(50)=9.36 microM for the RPMI-8226 leukemia cell line, and a GI(50)=0.552 microM and LC(50)=26.8 microM for the HOP-92 non-small cell lung cancer cell line.
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