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Synthesis and anticancer activity of sclerophytin-inspired hydroisobenzofurans |
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| Authors: | T David Bateman Aarti L Joshi Kwangyul Moon Elena N Galitovskaya Meenakshi Upreti Timothy C Chambers Matthias C McIntosh |
| Institution: | 1. Department of Chemistry and Biochemistry, 119 Chemistry Building, University of Arkansas, Fayetteville, AR 72701, United States;2. Department of Biochemistry and Molecular Biology, University of Arkansas for Medical Sciences, 4301 West Markham St., Little Rock, AR 72205, United States |
| 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 IC50’s of 1–3 μM in growth inhibitory assays against KB3 cells. The NCI 60-cell line 5-dose assay for analog 6h revealed a GI50 = 0.148 μM and LC50 = 9.36 μM for the RPMI-8226 leukemia cell line, and a GI50 = 0.552 μM and LC50 = 26.8 μM for the HOP-92 non-small cell lung cancer cell line. |
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