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Anilinoquinazoline inhibitors of the RET kinase domain-elaboration of the 7-position.

dc.contributor.authorJordan, Allan M
dc.contributor.authorBegum, Habiba
dc.contributor.authorFairweather, Emma E
dc.contributor.authorFritzl, Samantha J R
dc.contributor.authorGoldberg, Kristin M
dc.contributor.authorHopkins, Gemma V
dc.contributor.authorHamilton, Niall M
dc.contributor.authorLyons, Amanda J
dc.contributor.authorMarch, H Nikki
dc.contributor.authorNewton, Rebecca
dc.contributor.authorSmall, Helen F
dc.contributor.authorVishwanath, S
dc.contributor.authorWaddell, Ian D
dc.contributor.authorWaszkowycz, Bohdan
dc.contributor.authorWatson, Amanda J
dc.contributor.authorOgilvie, Donald J
dc.date.accessioned2016-05-25T15:24:18Zen
dc.date.available2016-05-25T15:24:18Zen
dc.date.issued2016-06-01en
dc.identifier.citationAnilinoquinazoline inhibitors of the RET kinase domain-elaboration of the 7-position. 2016, 26 (11):2724-9 Bioorg Med Chem Letten
dc.identifier.issn1464-3405en
dc.identifier.pmid27086121en
dc.identifier.doi10.1016/j.bmcl.2016.03.100en
dc.identifier.urihttp://hdl.handle.net/10541/610718en
dc.description.abstractWe have previously reported a series of anilinoquinazoline derivatives as potent and selective biochemical inhibitors of the RET kinase domain. However, these derivatives displayed diminished cellular potency. Herein we describe further optimisation of the series through modification of their physicochemical properties, delivering improvements in cell potency. However, whilst cellular selectivity against key targets could be maintained, combining cell potency and acceptable pharmacokinetics proved challenging.
dc.language.isoenen
dc.rightsArchived with thanks to Bioorganic & medicinal chemistry lettersen
dc.titleAnilinoquinazoline inhibitors of the RET kinase domain-elaboration of the 7-position.en
dc.typeArticleen
dc.contributor.departmentDrug Discovery Unit, Cancer Research UK Manchester Institute, University of Manchester, Wilmslow Road, Manchesteren
dc.identifier.journalBioorganic & Medicinal Chemistry Lettersen
html.description.abstractWe have previously reported a series of anilinoquinazoline derivatives as potent and selective biochemical inhibitors of the RET kinase domain. However, these derivatives displayed diminished cellular potency. Herein we describe further optimisation of the series through modification of their physicochemical properties, delivering improvements in cell potency. However, whilst cellular selectivity against key targets could be maintained, combining cell potency and acceptable pharmacokinetics proved challenging.


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