ChloroquineV1, Main, Exploration, bibRecord, 001E04

Synthesis and chloroquine-enhancing activity of Na-deacetyl-ferrocenoyl-strychnobrasiline

Identifieur interne : 001E04 ( Main/Exploration ); précédent : 001E03; suivant : 001E05

Synthesis and chloroquine-enhancing activity of Na-deacetyl-ferrocenoyl-strychnobrasiline

Auteurs : Lydie Pélinski [France] ; Dorothée Razafimahefa [Madagascar] ; Marie-Thérèse Martin [France] ; David Ramanitrahasimbola [Madagascar] ; Philippe Rasoanaivo [Madagascar] ; Jacques Brocard [France]

Source :

Bioorganic and Medicinal Chemistry Letters [ 0960-894X ] ; 2005-02-15.

RBID : Hal:hal-00115540

English descriptors

mix :
- Chemosensitizing activity, Chemosensitizing activity., Na-deacetyl-ferrocenoyl strychnobrasiline, Strychnobrasiline.

Abstract

Several strychnobrasiline derivatives have been synthesized to overcome the lack of in vivo reversal activity of the parent compound. In the present study, Na-deacetyl-ferrocenoyl-strychnobrasiline was synthesized by condensing Na-deacetyl-strychnobrasiline with ferrocenic acid previously treated with oxalyl chloride. While the in vitro antiplasmodial activity of the test compound (IC50 = 4.83 lg/mL) was increased 15-fold compared to that of strychnobrasiline, and the in vitro enhancing activity was found to be similar to that of the parent compound, the compound was devoid of any in vivo potentiating effect, and an antagonistic effect was even observed at higher doses. Based on the overall results on the hemisynthesis of strychnobrasiline derivatives for better reversal activity, this strategy has appeared to be of little value for useful drugs.

Url:

https://hal.archives-ouvertes.fr/hal-00115540

DOI: 10.1016/j.bmcl.2004.11.067

Affiliations:

France, Madagascar

Links toward previous steps (curation, corpus...)

to stream Hal, to step Corpus: 000225
to stream Hal, to step Curation: 000225
to stream Hal, to step Checkpoint: 000239
to stream Main, to step Merge: 001E19
to stream Main, to step Curation: 001E04

Le document en format XML

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</hal:affiliation>
<country>Madagascar</country>
</affiliation>
</author>
<author><name sortKey="Brocard, Jacques" sort="Brocard, Jacques" uniqKey="Brocard J" first="Jacques" last="Brocard">Jacques Brocard</name>
<affiliation wicri:level="1"><hal:affiliation type="laboratory" xml:id="struct-3209" status="VALID">          <idno type="IdRef">161608809</idno>
          <idno type="ISNI">0000 0004 0368 3038</idno>
          <idno type="RNSR">200612828X</idno>
          <orgName>Unité de Catalyse et de Chimie du Solide - UMR 8181</orgName>
          <orgName type="acronym">UCCS</orgName>
          <desc>            <address>              <addrLine>Cité Scientifique - Bâtiment C3 59655 Villeneuve d'Ascq Cedex</addrLine>
              <country key="FR"></country>
            </address>
          </desc>
          <listRelation>            <relation active="#struct-56711" type="direct"></relation>
            <relation active="#struct-120930" type="direct"></relation>
            <relation active="#struct-300369" type="direct"></relation>
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          </listRelation>
        <tutelles><tutelle active="#struct-56711" type="direct"><org type="institution" xml:id="struct-56711" status="VALID">          <orgName>Université d'Artois</orgName>
          <orgName type="acronym">UA</orgName>
          <desc>            <address>              <addrLine>9 rue du Temple - BP 10665 - 62030 Arras cedex</addrLine>
              <country key="FR"></country>
            </address>
            <ref type="url">http://www.univ-artois.fr/</ref>
          </desc>
        </org>
</tutelle>
<tutelle active="#struct-120930" type="direct"><org type="institution" xml:id="struct-120930" status="VALID">          <orgName>Ecole Centrale de Lille</orgName>
          <desc>            <address>              <addrLine>Cité Scientifique - CS 20048 59651 Villeneuve d'Ascq Cedex</addrLine>
              <country key="FR"></country>
            </address>
            <ref type="url">http://www.ec-lille.fr/</ref>
          </desc>
        </org>
</tutelle>
<tutelle active="#struct-300369" type="direct"><org type="institution" xml:id="struct-300369" status="VALID">          <orgName>Ecole Nationale Supérieure de Chimie de Lille</orgName>
          <orgName type="acronym">ENSCL</orgName>
          <desc>            <address>              <addrLine>Cité ScientifiqueBât. C7Avenue MendeleïevCS 9010859652 VILLENEUVE D’ASCQ CEDEX</addrLine>
              <country key="FR"></country>
            </address>
            <ref type="url">http://www.ensc-lille.fr</ref>
          </desc>
        </org>
</tutelle>
<tutelle active="#struct-374570" type="direct"><org type="institution" xml:id="struct-374570" status="VALID">          <idno type="IdRef">223446556</idno>
          <orgName>Université de Lille</orgName>
          <date type="start">2018-01-01</date>
          <desc>            <address>              <addrLine>Lille</addrLine>
              <country key="FR"></country>
            </address>
            <ref type="url">https://www.univ-lille.fr/</ref>
          </desc>
        </org>
</tutelle>
<tutelle name="UMR8181" active="#struct-441569" type="direct"><org type="institution" xml:id="struct-441569" status="VALID">          <idno type="IdRef">02636817X</idno>
          <idno type="ISNI">0000000122597504</idno>
          <orgName>Centre National de la Recherche Scientifique</orgName>
          <orgName type="acronym">CNRS</orgName>
          <date type="start">1939-10-19</date>
          <desc>            <address>              <country key="FR"></country>
            </address>
            <ref type="url">http://www.cnrs.fr/</ref>
          </desc>
        </org>
</tutelle>
</tutelles>
</hal:affiliation>
<country>France</country>
</affiliation>
</author>
</analytic>
<idno type="DOI">10.1016/j.bmcl.2004.11.067</idno>
<series><title level="j">Bioorganic and Medicinal Chemistry Letters</title>
<idno type="ISSN">0960-894X</idno>
<imprint><date type="datePub">2005-02-15</date>
</imprint>
</series>
</biblStruct>
</sourceDesc>
</fileDesc>
<profileDesc><textClass><keywords scheme="mix" xml:lang="en"><term>Chemosensitizing activity</term>
<term>Chemosensitizing activity.</term>
<term>Na-deacetyl-ferrocenoyl strychnobrasiline</term>
<term>Strychnobrasiline</term>
</keywords>
</textClass>
</profileDesc>
</teiHeader>
<front><div type="abstract" xml:lang="en">              <p>Several strychnobrasiline derivatives have been synthesized to overcome the lack of in vivo reversal activity of the parent compound. In the present study, Na-deacetyl-ferrocenoyl-strychnobrasiline was synthesized by condensing Na-deacetyl-strychnobrasiline with ferrocenic acid previously treated with oxalyl chloride. While the in vitro antiplasmodial activity of the test compound (IC50 = 4.83 lg/mL) was increased 15-fold compared to that of strychnobrasiline, and the in vitro enhancing activity was found to be similar to that of the parent compound, the compound was devoid of any in vivo potentiating effect, and an antagonistic effect was even observed at higher doses. Based on the overall results on the hemisynthesis of strychnobrasiline derivatives for better reversal activity, this strategy has appeared to be of little value for useful drugs.</p>
            </div>
</front>
</TEI>
<affiliations><list><country><li>France</li>
<li>Madagascar</li>
</country>
</list>
<tree><country name="France"><noRegion><name sortKey="Pelinski, Lydie" sort="Pelinski, Lydie" uniqKey="Pelinski L" first="Lydie" last="Pélinski">Lydie Pélinski</name>
</noRegion>
<name sortKey="Brocard, Jacques" sort="Brocard, Jacques" uniqKey="Brocard J" first="Jacques" last="Brocard">Jacques Brocard</name>
<name sortKey="Martin, Marie Therese" sort="Martin, Marie Therese" uniqKey="Martin M" first="Marie-Thérèse" last="Martin">Marie-Thérèse Martin</name>
</country>
<country name="Madagascar"><noRegion><name sortKey="Razafimahefa, Dorothee" sort="Razafimahefa, Dorothee" uniqKey="Razafimahefa D" first="Dorothée" last="Razafimahefa">Dorothée Razafimahefa</name>
</noRegion>
<name sortKey="Ramanitrahasimbola, David" sort="Ramanitrahasimbola, David" uniqKey="Ramanitrahasimbola D" first="David" last="Ramanitrahasimbola">David Ramanitrahasimbola</name>
<name sortKey="Rasoanaivo, Philippe" sort="Rasoanaivo, Philippe" uniqKey="Rasoanaivo P" first="Philippe" last="Rasoanaivo">Philippe Rasoanaivo</name>
</country>
</tree>
</affiliations>
</record>

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Synthesis and chloroquine-enhancing activity of Na-deacetyl-ferrocenoyl-strychnobrasiline

Synthesis and chloroquine-enhancing activity of Na-deacetyl-ferrocenoyl-strychnobrasiline

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