Novel Imatinib Derivatives with Altered Specificity between Bcr-AbI and FMS, KIT, and PDGF Receptors

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dc.contributor.authorSkobridis, K.en
dc.contributor.authorKinigopoulou, M.en
dc.contributor.authorTheodorou, V.en
dc.contributor.authorGiannousi, E.en
dc.contributor.authorRussell, A.en
dc.contributor.authorChauhan, R.en
dc.contributor.authorSala, R.en
dc.contributor.authorBrownlow, N.en
dc.contributor.authorKiriakidis, S.en
dc.contributor.authorDomin, J.en
dc.contributor.authorTzakos, A. G.en
dc.contributor.authorDibb, N. J.en
dc.date.accessioned2015-11-24T16:42:53Z
dc.date.available2015-11-24T16:42:53Z
dc.identifier.issn1860-7179-
dc.identifier.urihttps://olympias.lib.uoi.gr/jspui/handle/123456789/8613
dc.rightsDefault Licence-
dc.subjectdrug designen
dc.subjectimatiniben
dc.subjectkinase inhibitorsen
dc.subjectoncogenesen
dc.subjectsynthesisen
dc.subjectchronic myeloid-leukemiaen
dc.subjectphenylamino-pyrimidine papen
dc.subjectkinase inhibitor sti571en
dc.subjecttyrosine kinaseen
dc.subjectc-kiten
dc.subjectphiladelphia-chromosomeen
dc.subjectactivating mutationsen
dc.subjectsti-571 inhibitionen
dc.subjectcrystal-structureen
dc.subjectstructural basisen
dc.titleNovel Imatinib Derivatives with Altered Specificity between Bcr-AbI and FMS, KIT, and PDGF Receptorsen
heal.abstractImatinib is a clinically important ATP analogue inhibitor that targets the tyrosine kinase domain of the intracellular AbI kinase and the PDGF receptor family. Imatinib has revolutionised the treatment of chronic myeloid leukaemia, which is caused by the oncogene Bcr-AbI and certain solid tumours that harbor oncogenic mutations of the PDGF receptor family. As a leading kinase inhibitor, imatinib also provides an excellent model system to investigate how changes in drug design impact biological activity, which is an important consideration for rational drug design. Herein we report a new series of imatinib derivatives that in general have greater activity against the family of PDGF receptors and poorer activity against AbI, as a result of modifications of the phenyl and N-methylpiperazine rings. These new compounds provide a platform for further drug development against the therapeutically important PDGF receptor family and they also provide insight into the engineering of drugs with altered biological activity.en
heal.accesscampus-
heal.fullTextAvailabilityTRUE-
heal.identifier.primaryDOI 10.1002/cmdc.200900394-
heal.identifier.secondary<Go to ISI>://000273725700014-
heal.identifier.secondaryhttp://onlinelibrary.wiley.com/doi/10.1002/cmdc.200900394/abstract-
heal.journalNameChemMedChemen
heal.journalTypepeer reviewed-
heal.languageen-
heal.publicationDate2010-
heal.publisherWiley-VCH Verlagen
heal.recordProviderΠανεπιστήμιο Ιωαννίνων. Σχολή Θετικών Επιστημών. Τμήμα Χημείαςel
heal.typejournalArticle-
heal.type.elΆρθρο Περιοδικούel
heal.type.enJournal articleen

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