https://m2.mtmt.hu/ hun 2026-09-21 20:51 JournalArticle 32287706 VALIDATED true Research Institute for Medicines (iMed.ULisboa), Faculty of Pharmacy, Universidade de Lisboa, Av. Prof. Gama Pinto, Lisbon, 1649-003, Portugal Department of Medical Microbiology, Albert Szent-Györgyi Health Center, Faculty of Medicine, University of Szeged, Semmelweis utca 6, Szeged, 6725, Hungary Centro de Estudos Moçambicanos e de Etnociências (CEMEC), Faculdade de Ciências Naturais e Matemática, Universidade Pedagógica Campus de Lhanguene, Av. De Moçambique, Maputo, 21402161, Mozambique LAQV@REQUIMTE/Department of Chemistry and Biochemistry, Faculty of Sciences, University of Porto, Rua do Campo Alegre, Porto, 4169-007, Portugal Cited By :7 Export Date: 9 June 2023 Correspondence Address: Ferreira, M.-J.U.; Research Institute for Medicines (iMed.ULisboa), Av. Prof. Gama Pinto, Portugal; email: mjuferreira@ff.ulisboa.pt Chemicals/CAS: cisplatin, 15663-27-1, 26035-31-4, 96081-74-2; doxorubicin, 23214-92-8, 25316-40-9; verapamil, 152-11-4, 52-53-9 Funding details: Fundação para a Ciência e a Tecnologia, FCT, GINOP-2.3.2-15-2016-00012, PD/BD/135291/2017, PTDC/MED-QUI/30591/2017 Funding details: Nemzeti Kutatási Fejlesztési és Innovációs Hivatal, NKFIH, 2019/2020 Funding text 1: Funding: This study was supported by Fundação para a Ciência e a Tecnologia (FCT), Portugal (projects: PTDC/MED-QUI/30591/2017, and SAICT-PAC/0019/2015;PhD grant PD/BD/135291/2017). The study was also supported by the GINOP-2.3.2-15-2016-00012 project (University of Szeged, Hungary) and the Bilateral Portuguese–Hungarian Science & Technology Cooperation (FCT/NKFIH, 2019/2020). Funding text 2: This study was supported by Funda??o para a Ci?ncia e a Tecnologia (FCT), Portugal (projects: PTDC/MED-QUI/30591/2017, and SAICT-PAC/0019/2015; PhD grant PD/BD/135291/2017). The study was also supported by the GINOP-2.3.2-15-2016-00012 project (University of Szeged, Hungary) and the Bilateral Portuguese?Hungarian Science & Technology Cooperation (FCT/NKFIH, 2019/2020). 0 false 2026-07-30T07:48:41.244+0000 2023-07-04T06:51:10.008+0000 2021-10-06T06:32:32.620+0000 true 10040261 Vigyikánné Váradi Anikó /api/admin/10040261 Admin true 10040261 2025-02-04T14:03:12.916+0000 2023-07-04T06:51:10.324+0000 true 10083973 Szalai Fruzsina /api/admin/10083973 Admin true true false true 24 24 /api/publicationtype/24 PublicationType 1 true 24 JournalArticle true 10000059 Article true 24 24 /api/publicationtype/24 PublicationType 1 true 24 JournalArticle /api/subtype/10000059 Szakcikk SubType 101 true 10000059 true 1 /api/category/1 Category true 1 Cardoso, David Exploring the Monoterpene Indole Alkaloid Scaffold for Reversing P-Glycoprotein-Mediated Multidrug Resistance in Cancer true true /api/journal/10024432 REVIEWED true false 10024432 false 10024432 true 1424-8247 Journal FOREIGN 14 9 862 862 31 2021 Dregamine (1), a major monoterpene indole alkaloid isolated from Tabernaemontana elegans, was submitted to chemical transformation of the ketone function, yielding 19 azines (3-21) and 11 semicarbazones (22-32) bearing aliphatic or aromatic substituents. Their structures were assigned mainly by 1D and 2D NMR (COSY, HMQC, and HMBC) experiments. Compounds 3-32 were evaluated as multidrug resistance (MDR) reversers through functional and chemosensitivity assays in a human ABCB1-transfected mouse T-lymphoma cell model, overexpressing P-glycoprotein. A significant increase of P-gp inhibitory activity was observed for most derivatives, mainly those containing azine moieties with aromatic substituents. Compounds with trimethoxyphenyl (17) or naphthyl motifs (18, 19) were among the most active, exhibiting strong inhibition at 0.2 mu M. Moreover, most of the derivatives showed selective antiproliferative effects toward resistant cells, having a collateral sensitivity effect. In drug combination assays, all compounds showed to interact synergistically with doxorubicin. Selected compounds (12, 17, 18, 20, and 29) were evaluated in the ATPase activity assay, in which all compounds but 12 behaved as inhibitors. To gather further insights on drug-receptor interactions, in silico studies were also addressed. 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class="author-name" mtid="10074640"><a href="/gui2/?type=authors&mode=browse&sel=10074640" target="_blank">Szemerédi Nikoletta (<span class="authorship-author-name">Szemerédi Nikoletta</span> <span class="authorAux-mtmt"> orvosi mikrobiológia</span>) </a> </span> <span class="author-affil"><span title="Szegedi Tudományegyetem">SZTE</span>/<span title="Szent-Györgyi Albert Orvostudományi Kar">SZAOK</span>/Orvosi Mikrobiológiai Intézet</span> ;&nbsp;&nbsp;&nbsp; <span class="author-name" mtid="10012633"><a href="/gui2/?type=authors&mode=browse&sel=10012633" target="_blank">Spengler Gabriella (<span class="authorship-author-name">Spengler Gabriella</span> <span class="authorAux-mtmt"> Orvosi mikrobiológia</span>) </a> </span> <span class="author-affil"><span title="Szegedi Tudományegyetem">SZTE</span>/<span title="Szent-Györgyi Albert Orvostudományi Kar">SZAOK</span>/Orvosi Mikrobiológiai Intézet</span> ;&nbsp;&nbsp;&nbsp; <span class="author-name" >Mulhovo Silva </span> ;&nbsp;&nbsp;&nbsp; <span class="author-name" >dos Santos Daniel </span> ;&nbsp;&nbsp;&nbsp; <span class="author-name" >Ferreira Maria-José ✉ </span> </div> </div> <div class="title"><a href="/gui2/?mode=browse&params=publication;32287706" target="_blank">Exploring the Monoterpene Indole Alkaloid Scaffold for Reversing P-Glycoprotein-Mediated Multidrug Resistance in Cancer</a></div> <div> <span class="journal-title">PHARMACEUTICALS</span> <span class="journal-issn">( <a target="_blank" href="https://portal.issn.org/resource/ISSN/1424-8247">1424-8247</a>)</span>: <span class="journal-volume">14</span> <span class="journal-issue">9</span> <span class="page"> Paper 862. 31 p. </span> <span class="year">(2021)</span> </div> <div class="pub-footer"> <span class="language" xmlns="http://www.w3.org/1999/html">Nyelv: Angol | </span> <span class="identifiers"> <span class="id identifier oa_GOLD" title=" Gold "> <a style="color:blue" title="10.3390/ph14090862" target="_blank" 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title="27790" target="_blank" href="http://publicatio.bibl.u-szeged.hu/27790"> SZTE Publicatio </a> </span> </span> <OnlyViewableByAuthor><div class="ratings"> <div class="journal-subject">Folyóirat szakterülete: Scopus - Drug Discovery&nbsp;&nbsp;&nbsp;SJR indikátor:&nbsp;Q1</div> <div class="journal-subject">Folyóirat szakterülete: Scopus - Pharmaceutical Science&nbsp;&nbsp;&nbsp;SJR indikátor:&nbsp;Q1</div> <div class="journal-subject">Folyóirat szakterülete: Scopus - Molecular Medicine&nbsp;&nbsp;&nbsp;SJR indikátor:&nbsp;Q2</div> </div></OnlyViewableByAuthor> <div class="publication-citation" style="margin-left: 0.5cm;"> <span title="Nyilvános idézőközlemények összesen, említések nélkül" class="citingPub-count">Nyilvános idéző összesen: 17</span> | Független: 7 | Függő: 10 | Nem jelölt: 0 | WoS jelölt: 17 | Scopus jelölt:&nbsp;15 | WoS/Scopus jelölt:&nbsp;17 | DOI jelölt:&nbsp;17 </div> <div class="publication-citation"> <a target="_blank" href="/api/publication?cond=citations.related;eq;32287706&sort=publishedYear,desc&sort=title"> Idézett közlemények száma: 7 </a> </div> <div class="mtid"><span class="long-pub-mtid">Közlemény: 32287706</span> | <span class="status-data status-VALIDATED"> Egyeztetett </span> Forrás Idéző | <span class="type-subtype">Folyóiratcikk ( Szakcikk ) </span> | <span class="pub-category">Tudományos</span> | <span class="publication-sourceOfData">kézi felvitel</span> </div> <div class="lastModified">Utolsó módosítás: 2023.07.04. 08:51 Szalai Fruzsina (SZTE admin5) </div> <pre class="comment" style="margin-top: 0; margin-bottom: 0;"><u>Megjegyzés</u>: Research Institute for Medicines (iMed.ULisboa), Faculty of Pharmacy, Universidade de Lisboa, Av. Prof. Gama Pinto, Lisbon, 1649-003, Portugal Department of Medical Microbiology, Albert Szent-Györgyi Health Center, Faculty of Medicine, University of Szeged, Semmelweis utca 6, Szeged, 6725, Hungary Centro de Estudos Moçambicanos e de Etnociências (...</pre> </div></div>