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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Autores principales: Martins, Ana, Csábi, József, Balázs, Attila, Kitka, Diána, Amaral, Leonard, Molnár, József, Simon, András, Tóth, Gábor, Hunyadi, Attila
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2013
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6269874/
https://www.ncbi.nlm.nih.gov/pubmed/24335576
http://dx.doi.org/10.3390/molecules181215255
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author Martins, Ana
Csábi, József
Balázs, Attila
Kitka, Diána
Amaral, Leonard
Molnár, József
Simon, András
Tóth, Gábor
Hunyadi, Attila
author_facet Martins, Ana
Csábi, József
Balázs, Attila
Kitka, Diána
Amaral, Leonard
Molnár, József
Simon, András
Tóth, Gábor
Hunyadi, Attila
author_sort Martins, Ana
collection PubMed
description 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 (1)H- and (13)C-NMR signal assignment.
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spelling pubmed-62698742018-12-20 Synthesis and Structure-Activity Relationships of Novel Ecdysteroid Dioxolanes as MDR Modulators in Cancer Martins, Ana Csábi, József Balázs, Attila Kitka, Diána Amaral, Leonard Molnár, József Simon, András Tóth, Gábor Hunyadi, Attila Molecules Article 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 (1)H- and (13)C-NMR signal assignment. MDPI 2013-12-10 /pmc/articles/PMC6269874/ /pubmed/24335576 http://dx.doi.org/10.3390/molecules181215255 Text en © 2013 by the authors; licensee MDPI, Basel, Switzerland. http://creativecommons.org/licenses/by/3.0/ This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Article
Martins, Ana
Csábi, József
Balázs, Attila
Kitka, Diána
Amaral, Leonard
Molnár, József
Simon, András
Tóth, Gábor
Hunyadi, Attila
Synthesis and Structure-Activity Relationships of Novel Ecdysteroid Dioxolanes as MDR Modulators in Cancer
title Synthesis and Structure-Activity Relationships of Novel Ecdysteroid Dioxolanes as MDR Modulators in Cancer
title_full Synthesis and Structure-Activity Relationships of Novel Ecdysteroid Dioxolanes as MDR Modulators in Cancer
title_fullStr Synthesis and Structure-Activity Relationships of Novel Ecdysteroid Dioxolanes as MDR Modulators in Cancer
title_full_unstemmed Synthesis and Structure-Activity Relationships of Novel Ecdysteroid Dioxolanes as MDR Modulators in Cancer
title_short Synthesis and Structure-Activity Relationships of Novel Ecdysteroid Dioxolanes as MDR Modulators in Cancer
title_sort synthesis and structure-activity relationships of novel ecdysteroid dioxolanes as mdr modulators in cancer
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6269874/
https://www.ncbi.nlm.nih.gov/pubmed/24335576
http://dx.doi.org/10.3390/molecules181215255
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