Discovery of 1-(4-(5-(5-amino-6-(5-tert-butyl-1,3,4-oxadiazol-2-yl)pyrazin-2-yl)-1-ethyl-1,2,4-triazol-3-yl)piperidin-1-yl)-3-hydroxypropan-1-one (AZD8835): A potent and selective inhibitor of PI3Kα and PI3Kδ for the treatment of cancers.
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| Title: | Discovery of 1-(4-(5-(5-amino-6-(5-tert-butyl-1,3,4-oxadiazol-2-yl)pyrazin-2-yl)-1-ethyl-1,2,4-triazol-3-yl)piperidin-1-yl)-3-hydroxypropan-1-one (AZD8835): A potent and selective inhibitor of PI3Kα and PI3Kδ for the treatment of cancers. |
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| Authors: | Barlaam B; AstraZeneca, Oncology iMed, Alderley Park, Macclesfield, Cheshire SK10 4TG, United Kingdom. Electronic address: bernard.barlaam2@astrazeneca.com., Cosulich S; AstraZeneca, Oncology iMed, Alderley Park, Macclesfield, Cheshire SK10 4TG, United Kingdom., Delouvrié B; AstraZeneca, Centre de Recherches, Z.I. La Pompelle, B.P. 1050, Chemin de Vrilly, 51689 Reims Cedex 2, France., Ellston R; AstraZeneca, Oncology iMed, Alderley Park, Macclesfield, Cheshire SK10 4TG, United Kingdom., Fitzek M; AstraZeneca, Oncology iMed, Alderley Park, Macclesfield, Cheshire SK10 4TG, United Kingdom., Germain H; AstraZeneca, Centre de Recherches, Z.I. La Pompelle, B.P. 1050, Chemin de Vrilly, 51689 Reims Cedex 2, France., Green S; AstraZeneca, Oncology iMed, Alderley Park, Macclesfield, Cheshire SK10 4TG, United Kingdom., Hancox U; AstraZeneca, Oncology iMed, Alderley Park, Macclesfield, Cheshire SK10 4TG, United Kingdom., Harris CS; AstraZeneca, Centre de Recherches, Z.I. La Pompelle, B.P. 1050, Chemin de Vrilly, 51689 Reims Cedex 2, France., Hudson K; AstraZeneca, Oncology iMed, Alderley Park, Macclesfield, Cheshire SK10 4TG, United Kingdom., Lambert-van der Brempt C; AstraZeneca, Centre de Recherches, Z.I. La Pompelle, B.P. 1050, Chemin de Vrilly, 51689 Reims Cedex 2, France., Lebraud H; AstraZeneca, Centre de Recherches, Z.I. La Pompelle, B.P. 1050, Chemin de Vrilly, 51689 Reims Cedex 2, France., Magnien F; AstraZeneca, Centre de Recherches, Z.I. La Pompelle, B.P. 1050, Chemin de Vrilly, 51689 Reims Cedex 2, France., Lamorlette M; AstraZeneca, Centre de Recherches, Z.I. La Pompelle, B.P. 1050, Chemin de Vrilly, 51689 Reims Cedex 2, France., Le Griffon A; AstraZeneca, Centre de Recherches, Z.I. La Pompelle, B.P. 1050, Chemin de Vrilly, 51689 Reims Cedex 2, France., Morgentin R; AstraZeneca, Centre de Recherches, Z.I. La Pompelle, B.P. 1050, Chemin de Vrilly, 51689 Reims Cedex 2, France., Ouvry G; AstraZeneca, Centre de Recherches, Z.I. La Pompelle, B.P. 1050, Chemin de Vrilly, 51689 Reims Cedex 2, France., Page K; AstraZeneca, Oncology iMed, Alderley Park, Macclesfield, Cheshire SK10 4TG, United Kingdom., Pasquet G; AstraZeneca, Centre de Recherches, Z.I. La Pompelle, B.P. 1050, Chemin de Vrilly, 51689 Reims Cedex 2, France., Polanska U; AstraZeneca, Oncology iMed, Alderley Park, Macclesfield, Cheshire SK10 4TG, United Kingdom., Ruston L; AstraZeneca, Oncology iMed, Alderley Park, Macclesfield, Cheshire SK10 4TG, United Kingdom., Saleh T; AstraZeneca, Centre de Recherches, Z.I. La Pompelle, B.P. 1050, Chemin de Vrilly, 51689 Reims Cedex 2, France., Vautier M; AstraZeneca, Centre de Recherches, Z.I. La Pompelle, B.P. 1050, Chemin de Vrilly, 51689 Reims Cedex 2, France., Ward L; AstraZeneca, Oncology iMed, Alderley Park, Macclesfield, Cheshire SK10 4TG, United Kingdom. |
| Source: | Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2015 Nov 15; Vol. 25 (22), pp. 5155-62. Date of Electronic Publication: 2015 Oct 09. |
| Publication Type: | Journal Article |
| Journal Info: | Publisher: Elsevier Science Ltd Country of Publication: England NLM ID: 9107377 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1464-3405 (Electronic) Linking ISSN: 0960894X NLM ISO Abbreviation: Bioorg Med Chem Lett Subsets: MEDLINE |
| Database: | MEDLINE Ultimate |
| FullText | Text: Availability: 0 |
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| Header | DbId: mdl DbLabel: MEDLINE Ultimate An: 26475521 AccessLevel: 2 PubType: Academic Journal PubTypeId: academicJournal PreciseRelevancyScore: 0 |
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| Items | – Name: Title Label: Title Group: Ti Data: Discovery of 1-(4-(5-(5-amino-6-(5-tert-butyl-1,3,4-oxadiazol-2-yl)pyrazin-2-yl)-1-ethyl-1,2,4-triazol-3-yl)piperidin-1-yl)-3-hydroxypropan-1-one (AZD8835): A potent and selective inhibitor of PI3Kα and PI3Kδ for the treatment of cancers. – Name: Author Label: Authors Group: Au Data: <searchLink fieldCode="AU" term="%22Barlaam+B%22">Barlaam B</searchLink>; AstraZeneca, Oncology iMed, Alderley Park, Macclesfield, Cheshire SK10 4TG, United Kingdom. Electronic address: bernard.barlaam2@astrazeneca.com.<br /><searchLink fieldCode="AU" term="%22Cosulich+S%22">Cosulich S</searchLink>; AstraZeneca, Oncology iMed, Alderley Park, Macclesfield, Cheshire SK10 4TG, United Kingdom.<br /><searchLink fieldCode="AU" term="%22Delouvrié+B%22">Delouvrié B</searchLink>; AstraZeneca, Centre de Recherches, Z.I. La Pompelle, B.P. 1050, Chemin de Vrilly, 51689 Reims Cedex 2, France.<br /><searchLink fieldCode="AU" term="%22Ellston+R%22">Ellston R</searchLink>; AstraZeneca, Oncology iMed, Alderley Park, Macclesfield, Cheshire SK10 4TG, United Kingdom.<br /><searchLink fieldCode="AU" term="%22Fitzek+M%22">Fitzek M</searchLink>; AstraZeneca, Oncology iMed, Alderley Park, Macclesfield, Cheshire SK10 4TG, United Kingdom.<br /><searchLink fieldCode="AU" term="%22Germain+H%22">Germain H</searchLink>; AstraZeneca, Centre de Recherches, Z.I. La Pompelle, B.P. 1050, Chemin de Vrilly, 51689 Reims Cedex 2, France.<br /><searchLink fieldCode="AU" term="%22Green+S%22">Green S</searchLink>; AstraZeneca, Oncology iMed, Alderley Park, Macclesfield, Cheshire SK10 4TG, United Kingdom.<br /><searchLink fieldCode="AU" term="%22Hancox+U%22">Hancox U</searchLink>; AstraZeneca, Oncology iMed, Alderley Park, Macclesfield, Cheshire SK10 4TG, United Kingdom.<br /><searchLink fieldCode="AU" term="%22Harris+CS%22">Harris CS</searchLink>; AstraZeneca, Centre de Recherches, Z.I. La Pompelle, B.P. 1050, Chemin de Vrilly, 51689 Reims Cedex 2, France.<br /><searchLink fieldCode="AU" term="%22Hudson+K%22">Hudson K</searchLink>; AstraZeneca, Oncology iMed, Alderley Park, Macclesfield, Cheshire SK10 4TG, United Kingdom.<br /><searchLink fieldCode="AU" term="%22Lambert-van+der+Brempt+C%22">Lambert-van der Brempt C</searchLink>; AstraZeneca, Centre de Recherches, Z.I. La Pompelle, B.P. 1050, Chemin de Vrilly, 51689 Reims Cedex 2, France.<br /><searchLink fieldCode="AU" term="%22Lebraud+H%22">Lebraud H</searchLink>; AstraZeneca, Centre de Recherches, Z.I. La Pompelle, B.P. 1050, Chemin de Vrilly, 51689 Reims Cedex 2, France.<br /><searchLink fieldCode="AU" term="%22Magnien+F%22">Magnien F</searchLink>; AstraZeneca, Centre de Recherches, Z.I. La Pompelle, B.P. 1050, Chemin de Vrilly, 51689 Reims Cedex 2, France.<br /><searchLink fieldCode="AU" term="%22Lamorlette+M%22">Lamorlette M</searchLink>; AstraZeneca, Centre de Recherches, Z.I. La Pompelle, B.P. 1050, Chemin de Vrilly, 51689 Reims Cedex 2, France.<br /><searchLink fieldCode="AU" term="%22Le+Griffon+A%22">Le Griffon A</searchLink>; AstraZeneca, Centre de Recherches, Z.I. La Pompelle, B.P. 1050, Chemin de Vrilly, 51689 Reims Cedex 2, France.<br /><searchLink fieldCode="AU" term="%22Morgentin+R%22">Morgentin R</searchLink>; AstraZeneca, Centre de Recherches, Z.I. La Pompelle, B.P. 1050, Chemin de Vrilly, 51689 Reims Cedex 2, France.<br /><searchLink fieldCode="AU" term="%22Ouvry+G%22">Ouvry G</searchLink>; AstraZeneca, Centre de Recherches, Z.I. La Pompelle, B.P. 1050, Chemin de Vrilly, 51689 Reims Cedex 2, France.<br /><searchLink fieldCode="AU" term="%22Page+K%22">Page K</searchLink>; AstraZeneca, Oncology iMed, Alderley Park, Macclesfield, Cheshire SK10 4TG, United Kingdom.<br /><searchLink fieldCode="AU" term="%22Pasquet+G%22">Pasquet G</searchLink>; AstraZeneca, Centre de Recherches, Z.I. La Pompelle, B.P. 1050, Chemin de Vrilly, 51689 Reims Cedex 2, France.<br /><searchLink fieldCode="AU" term="%22Polanska+U%22">Polanska U</searchLink>; AstraZeneca, Oncology iMed, Alderley Park, Macclesfield, Cheshire SK10 4TG, United Kingdom.<br /><searchLink fieldCode="AU" term="%22Ruston+L%22">Ruston L</searchLink>; AstraZeneca, Oncology iMed, Alderley Park, Macclesfield, Cheshire SK10 4TG, United Kingdom.<br /><searchLink fieldCode="AU" term="%22Saleh+T%22">Saleh T</searchLink>; AstraZeneca, Centre de Recherches, Z.I. La Pompelle, B.P. 1050, Chemin de Vrilly, 51689 Reims Cedex 2, France.<br /><searchLink fieldCode="AU" term="%22Vautier+M%22">Vautier M</searchLink>; AstraZeneca, Centre de Recherches, Z.I. La Pompelle, B.P. 1050, Chemin de Vrilly, 51689 Reims Cedex 2, France.<br /><searchLink fieldCode="AU" term="%22Ward+L%22">Ward L</searchLink>; AstraZeneca, Oncology iMed, Alderley Park, Macclesfield, Cheshire SK10 4TG, United Kingdom. – Name: TitleSource Label: Source Group: Src Data: <searchLink fieldCode="JN" term="%229107377%22">Bioorganic & medicinal chemistry letters</searchLink> [Bioorg Med Chem Lett] 2015 Nov 15; Vol. 25 (22), pp. 5155-62. <i>Date of Electronic Publication: </i>2015 Oct 09. – Name: TypePub Label: Publication Type Group: TypPub Data: Journal Article – Name: TitleSource Label: Journal Info Group: Src Data: <i>Publisher: </i><searchLink fieldCode="PB" term="%22Elsevier+Science+Ltd%22">Elsevier Science Ltd </searchLink><i>Country of Publication: </i>England <i>NLM ID: </i>9107377 <i>Publication Model: </i>Print-Electronic <i>Cited Medium: </i>Internet <i>ISSN: </i>1464-3405 (Electronic) <i>Linking ISSN: </i><searchLink fieldCode="IS" term="%220960894X%22">0960894X </searchLink><i>NLM ISO Abbreviation: </i>Bioorg Med Chem Lett <i>Subsets: </i>MEDLINE |
| PLink | https://search.ebscohost.com/login.aspx?direct=true&site=eds-live&db=mdl&AN=26475521 |
| RecordInfo | BibRecord: BibEntity: Identifiers: – Type: doi Value: 10.1016/j.bmcl.2015.10.002 Languages: – Code: eng Text: English PhysicalDescription: Pagination: StartPage: 5155 Titles: – TitleFull: Discovery of 1-(4-(5-(5-amino-6-(5-tert-butyl-1,3,4-oxadiazol-2-yl)pyrazin-2-yl)-1-ethyl-1,2,4-triazol-3-yl)piperidin-1-yl)-3-hydroxypropan-1-one (AZD8835): A potent and selective inhibitor of PI3Kα and PI3Kδ for the treatment of cancers. Type: main BibRelationships: HasContributorRelationships: – PersonEntity: Name: NameFull: Barlaam B – PersonEntity: Name: NameFull: Cosulich S – PersonEntity: Name: NameFull: Delouvrié B – PersonEntity: Name: NameFull: Ellston R – PersonEntity: Name: NameFull: Fitzek M – PersonEntity: Name: NameFull: Germain H – PersonEntity: Name: NameFull: Green S – PersonEntity: Name: NameFull: Hancox U – PersonEntity: Name: NameFull: Harris CS – PersonEntity: Name: NameFull: Hudson K – PersonEntity: Name: NameFull: Lambert-van der Brempt C – PersonEntity: Name: NameFull: Lebraud H – PersonEntity: Name: NameFull: Magnien F – PersonEntity: Name: NameFull: Lamorlette M – PersonEntity: Name: NameFull: Le Griffon A – PersonEntity: Name: NameFull: Morgentin R – PersonEntity: Name: NameFull: Ouvry G – PersonEntity: Name: NameFull: Page K – PersonEntity: Name: NameFull: Pasquet G – PersonEntity: Name: NameFull: Polanska U – PersonEntity: Name: NameFull: Ruston L – PersonEntity: Name: NameFull: Saleh T – PersonEntity: Name: NameFull: Vautier M – PersonEntity: Name: NameFull: Ward L IsPartOfRelationships: – BibEntity: Dates: – D: 15 M: 11 Text: 2015 Nov 15 Type: published Y: 2015 Identifiers: – Type: issn-electronic Value: 1464-3405 Numbering: – Type: volume Value: 25 – Type: issue Value: 22 Titles: – TitleFull: Bioorganic & medicinal chemistry letters Type: main |
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