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A combined ligand- and structure-based approach for the identification of rilmenidine-derived compounds which synergize the antitumor effects of doxorubicin
dc.creator | Vučićević, Jelica | |
dc.creator | Srdić-Rajić, Tatjana | |
dc.creator | Pieroni, Marco | |
dc.creator | Laurila, Jonne M. M. | |
dc.creator | Perović, Vladimir R. | |
dc.creator | Tassini, Sabrina | |
dc.creator | Azzali, Elisa | |
dc.creator | Costantino, Gabriele | |
dc.creator | Glišić, Sanja | |
dc.creator | Agbaba, Danica | |
dc.creator | Scheinin, Mika | |
dc.creator | Nikolić, Katarina M. | |
dc.creator | Radi, Marco | |
dc.creator | Veljković, Nevena V. | |
dc.date.accessioned | 2018-03-01T16:57:00Z | |
dc.date.available | 2018-03-01T16:57:00Z | |
dc.date.issued | 2016 | |
dc.identifier.issn | 0968-0896 | |
dc.identifier.uri | https://vinar.vin.bg.ac.rs/handle/123456789/1110 | |
dc.description.abstract | The clonidine-like central antihypertensive agent rilmenidine, which has high affinity for I-1-type imidazoline receptors (I-1-IR) was recently found to have cytotoxic effects on cultured cancer cell lines. However, due to its pharmacological effects resulting also from alpha(2)-adrenoceptor activation, rilmenidine cannot be considered a suitable anticancer drug candidate. Here, we report the identification of novel rilmenidine- derived compounds with anticancer potential and devoid of alpha(2)-adrenoceptor effects by means of ligand-and structure-based drug design approaches. Starting from a large virtual library, eleven compounds were selected, synthesized and submitted to biological evaluation. The most active compound 5 exhibited a cytotoxic profile similar to that of rilmenidine, but without appreciable affinity to alpha(2)-adrenoceptors. In addition, compound 5 significantly enhanced the apoptotic response to doxorubicin, and may thus represent an important tool for the development of better adjuvant chemotherapeutic strategies for doxorubicin-insensitive cancers. (C) 2016 Elsevier Ltd. All rights reserved. | en |
dc.relation | info:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/173001/RS// | |
dc.relation | info:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172033/RS// | |
dc.relation | University of Parma, Italy, Turku University Hospital, Finland, Chiesi Foundation | |
dc.rights | restrictedAccess | en |
dc.source | Bioorganic and Medicinal Chemistry | en |
dc.subject | Drug design | en |
dc.subject | Synthesis | en |
dc.subject | Rilmenidine | en |
dc.subject | Doxorubicin synergism | en |
dc.subject | alpha(2)-Adrenoceptors | en |
dc.subject | Cytotoxic activity | en |
dc.subject | Apoptosis | en |
dc.title | A combined ligand- and structure-based approach for the identification of rilmenidine-derived compounds which synergize the antitumor effects of doxorubicin | en |
dc.type | article | en |
dc.rights.license | ARR | |
dcterms.abstract | Цостантино, Габриеле; Срдиц-Рајиц, Татјана; Вуцицевиц, Јелица; Перовић Владимир; Aгбаба, Даница; Aззали, Елиса; Лаурила, Јонне М. М.; Глишић Сања; Сцхеинин, Мика; Ради, Марцо; Николиц, Катарина; Вељковић Невена В.; Тассини, Сабрина; Пиерони, Марцо; | |
dc.rights.holder | © 2016 Elsevier Ltd | |
dc.citation.volume | 24 | |
dc.citation.issue | 14 | |
dc.citation.spage | 3174 | |
dc.citation.epage | 3183 | |
dc.identifier.wos | 000377469800011 | |
dc.identifier.doi | 10.1016/j.bmc.2016.05.043 | |
dc.citation.rank | M21 | |
dc.identifier.pmid | 27265687 | |
dc.type.version | publishedVersion | |
dc.identifier.scopus | 2-s2.0-84975807224 |
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180 - Laboratorija za bioinformatiku i računarsku hemiju
Department of Bioinformatics and Computational Chemistry