Abstract
Ecdysteroids, molting hormones of insects, can exert several mild, non-hormonal bioactivities in mammals, including humans. In a previous study, we have found a significant effect of certain derivatives on the ABCB1 transporter mediated multi-drug resistance of a transfected murine leukemia cell line. In this paper, we present a structure-activity relationship study focused on the apolar dioxolane derivatives of 20-hydroxyecdysone. Semi-synthesis and bioactivity of a total of 32 ecdysteroids, including 20 new compounds, is presented, supplemented with their complete 1H- and 13C-NMR signal assignment.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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ATP Binding Cassette Transporter, Subfamily B / antagonists & inhibitors*
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Animals
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Antineoplastic Agents / pharmacology
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Cell Line, Tumor
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Cell Proliferation / drug effects
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Combinatorial Chemistry Techniques
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Dioxolanes / chemical synthesis
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Dioxolanes / chemistry*
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Dioxolanes / pharmacology*
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Doxorubicin / pharmacology
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Drug Synergism
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Ecdysteroids / chemical synthesis
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Ecdysteroids / chemistry*
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Ecdysteroids / pharmacology*
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Inhibitory Concentration 50
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Lymphoma / metabolism
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Mice
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Molecular Structure
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Neoplasms / metabolism*
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Nuclear Magnetic Resonance, Biomolecular
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Structure-Activity Relationship
Substances
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ATP Binding Cassette Transporter, Subfamily B
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Antineoplastic Agents
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Dioxolanes
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Ecdysteroids
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Doxorubicin
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formal glycol