2,3,5-Trisubstituted pyridines as selective AKT inhibitors—Part I: Substitution at 2-position of the core pyridine for ROCK1 selectivity
- Author
- HONG LIN1 ; YAMASHITA, DennisS1 ; ZHIHONG LAI2 ; MINTHORN, Elisabeth A3 ; STRUM, Susan L4 ; WOOD, Edgar R4 ; ELKINS, Patricia A4 ; CONCHA, Nestor O4 ; HEERDING, Dirk A1 ; JIN ZENG1 ; REN XIE1 ; WENYONG WANG1 ; NIDARMARTHY, Sirishkumar1 ; LUENGO, Juan I1 ; RHODES, Nelson2 ; KNICK, Victoria B2 ; CHOUDHRY, Anthony E2
[1] Oncology Medicinal Chemistry, GlaxoSmithKline, 1250 S. Collegeville, Rd., Collegeville, PA 19426, United States
[2] Oncology Biology, GlaxoSmithKline, 1250 S. Collegeville, Rd., Collegeville, PA 19426, United States
[3] Oncology Drug Metabolism and Pharmacokinetics, GlaxoSmithKline, 1250 S. Collegeville, Rd., Collegeville, PA 19426, United States
[4] Molecular Discovery Research, GlaxoSmithKline, 1250 S. Collegeville, Rd., Collegeville, PA 19426, United States - Source
Bioorganic & medicinal chemistry letters (Print). 2010, Vol 20, Num 2, pp 673-678, 6 p
- ISSN
- 0960-894X
- Scientific domain
- Biochemistry, molecular biology, biophysics; Pharmacology drugs
- Publisher
- Elsevier, Amsterdam
- Publication country
- Netherlands
- Document type
- Article
- Language
- English
- Author keyword
- AKT kinase inhibitors Selectivity
- Keyword (fr)
- Akt protein kinase Aminoéther Complexe enzyme inhibiteur Diffraction RX Dérivé de l'indazole Dérivé de l'indole Dérivé de la pyridine Dérivé du furane In vitro Inhibiteur enzyme Non-specific serine/threonine protein kinase Relation structure activité Structure cristalline Structure moléculaire Synthèse chimique Sélectivité Transduction signal Inhibiteur akt protein kinase Enzyme Transferases
- Keyword (en)
- Akt protein kinase Aminoether Inhibitor enzyme complex X ray diffraction Indazole derivatives Indole derivatives Pyridine derivatives Furan derivatives In vitro Enzyme inhibitor Non-specific serine/threonine protein kinase Structure activity relation Crystalline structure Molecular structure Chemical synthesis Selectivity Signal transduction Enzyme Transferases
- Keyword (es)
- Akt protein kinase Aminoeter Complejo enzima inhibidor Difracción RX Indazol derivado Indol derivado Piridina derivado Furano derivado In vitro Inhibidor enzima Non-specific serine/threonine protein kinase Relación estructura actividad Estructura cristalina Estructura molecular Síntesis química Selectividad Transducción señal Enzima Transferases
- Classification
- Pascal
- 002 Biological and medical sciences / 002B Medical sciences / 002B02 Pharmacology. Drug treatments / 002B02R Antineoplastic agents / 002B02R01 General aspects
- Discipline
- Pharmacological treatments
- Origin
- Inist-CNRS
- Database
- PASCAL
- INIST identifier
- 22389495
Sauf mention contraire ci-dessus, le contenu de cette notice bibliographique peut être utilisé dans le cadre d’une licence CC BY 4.0 Inist-CNRS / Unless otherwise stated above, the content of this bibliographic record may be used under a CC BY 4.0 licence by Inist-CNRS / A menos que se haya señalado antes, el contenido de este registro bibliográfico puede ser utilizado al amparo de una licencia CC BY 4.0 Inist-CNRS
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DOI
10.1016/j.bmcl.2009.11.064 
https://dx.doi.org/10.1016/j.bmcl.2009.11.064
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