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dc.creatorVučićević, Jelica
dc.creatorSrdić-Rajić, Tatjana
dc.creatorPieroni, Marco
dc.creatorLaurila, Jonne M. M.
dc.creatorPerović, Vladimir
dc.creatorTassini, Sabrina
dc.creatorAzzali, Elisa
dc.creatorCostantino, Gabriele
dc.creatorGlisić, Sanja
dc.creatorAgbaba, Danica
dc.creatorScheinin, Mika
dc.creatorNikolić, Katarina
dc.creatorRadi, Marco
dc.creatorVeljković, Nevena
dc.date.accessioned2019-09-02T11:50:20Z
dc.date.available2019-09-02T11:50:20Z
dc.date.issued2016
dc.identifier.issn0968-0896
dc.identifier.urihttp://farfar.pharmacy.bg.ac.rs/handle/123456789/2526
dc.description.abstractThe 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.en
dc.publisherPergamon-Elsevier Science Ltd, Oxford
dc.relationinfo:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172033/RS//
dc.relationinfo:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/173001/RS//
dc.relationChiesi Foundation
dc.relationTurku University Hospital, Finland
dc.relationUniversity of Parma, Italy
dc.rightsrestrictedAccess
dc.sourceBioorganic & Medicinal Chemistry
dc.titleA combined ligand- and structure-based approach for the identification of rilmenidine-derived compounds which synergize the antitumor effects of doxorubicinen
dc.typearticle
dc.rights.licenseARR
dcterms.abstractСрдић-Рајић, Татјана; Aззали, Елиса; Глисић, Сања; Сцхеинин, Мика; Перовић, Владимир; Николић, Катарина; Вучићевић, Јелица; Цостантино, Габриеле; Вељковић, Невена; Aгбаба, Даница; Ради, Марцо; Пиерони, Марцо; Лаурила, Јонне М. М.; Тассини, Сабрина;
dc.citation.volume24
dc.citation.issue14
dc.citation.spage3174
dc.citation.epage3183
dc.citation.other24(14): 3174-3183
dc.citation.rankM21
dc.identifier.wos000377469800011
dc.identifier.doi10.1016/j.bmc.2016.05.043
dc.identifier.pmid27265687
dc.identifier.scopus2-s2.0-84975807224
dc.identifier.rcubconv_3589
dc.type.versionpublishedVersion


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