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dc.creatorVučićević, Jelica
dc.creatorSrdić-Rajić, Tatjana
dc.creatorPieroni, Marco
dc.creatorLaurila, Jonne M. M.
dc.creatorPerović, Vladimir R.
dc.creatorTassini, Sabrina
dc.creatorAzzali, Elisa
dc.creatorCostantino, Gabriele
dc.creatorGlišić, Sanja
dc.creatorAgbaba, Danica
dc.creatorScheinin, Mika
dc.creatorNikolić, Katarina M.
dc.creatorRadi, Marco
dc.creatorVeljković, Nevena V.
dc.date.accessioned2018-03-01T16:57:00Z
dc.date.available2018-03-01T16:57:00Z
dc.date.issued2016
dc.identifier.issn0968-0896
dc.identifier.urihttps://vinar.vin.bg.ac.rs/handle/123456789/1110
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. (C) 2016 Elsevier Ltd. All rights reserved.en
dc.relationinfo:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/173001/RS//
dc.relationinfo:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172033/RS//
dc.relationUniversity of Parma, Italy, Turku University Hospital, Finland, Chiesi Foundation
dc.rightsrestrictedAccessen
dc.sourceBioorganic and Medicinal Chemistryen
dc.subjectDrug designen
dc.subjectSynthesisen
dc.subjectRilmenidineen
dc.subjectDoxorubicin synergismen
dc.subjectalpha(2)-Adrenoceptorsen
dc.subjectCytotoxic activityen
dc.subjectApoptosisen
dc.titleA combined ligand- and structure-based approach for the identification of rilmenidine-derived compounds which synergize the antitumor effects of doxorubicinen
dc.typearticleen
dc.rights.licenseARR
dcterms.abstractЦостантино, 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.volume24
dc.citation.issue14
dc.citation.spage3174
dc.citation.epage3183
dc.identifier.wos000377469800011
dc.identifier.doi10.1016/j.bmc.2016.05.043
dc.citation.rankM21
dc.identifier.pmid27265687
dc.type.versionpublishedVersion
dc.identifier.scopus2-s2.0-84975807224


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