Synthesis and structure-activity relationships of novel ecdysteroid dioxolanes as MDR modulators in cancer

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 lin...

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Veröffentlicht in:	Molecules (Basel, Switzerland) Switzerland), 2013-12, Vol.18 (12), p.15255-15275
Hauptverfasser:	Martins, Ana, Csábi, József, Balázs, Attila, Kitka, Diána, Amaral, Leonard, Molnár, József, Simon, András, Tóth, Gábor, Hunyadi, Attila
Format:	Artikel
Sprache:	eng
Schlagworte:	20-hydroxyecdysone ABCB1 transporter acetonide Animals Antineoplastic Agents - pharmacology Arthropods ATP Binding Cassette Transporter, Subfamily B - antagonists & inhibitors Cancer Carbon Cell Line, Tumor Cell Proliferation - drug effects Combinatorial Chemistry Techniques dioxolane Dioxolanes - chemical synthesis Dioxolanes - chemistry Dioxolanes - pharmacology Doxorubicin - pharmacology Drug resistance Drug Synergism ecdysteroids Ecdysteroids - chemical synthesis Ecdysteroids - chemistry Ecdysteroids - pharmacology efflux pump Electronic mail systems Hormones Inhibitory Concentration 50 Leukemia Lymphoma - metabolism Mice Molecular Structure multi-drug resistance Neoplasms - metabolism Nuclear Magnetic Resonance, Biomolecular P-glycoprotein stereochemistry Steroids Structure-Activity Relationship Tropical diseases
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Beschreibung
Zusammenfassung:	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.
ISSN:	1420-3049 1420-3049
DOI:	10.3390/molecules181215255