✦ LIBER ✦

Structure-based design of imidazo[1,2-a]pyrazine derivatives as selective inhibitors of Aurora-A kinase in cells

✍ Scribed by Nathalie Bouloc; Jonathan M. Large; Magda Kosmopoulou; Chongbo Sun; Amir Faisal; Mizio Matteucci; Jóhannes Reynisson; Nathan Brown; Butrus Atrash; Julian Blagg; Edward McDonald; Spiros Linardopoulos; Richard Bayliss; Vassilios Bavetsias

Book ID: 104004813
Publisher: Elsevier Science
Year: 2010
Tongue: English
Weight: 879 KB
Volume: 20
Category: Article
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2010.08.091

No coin nor oath required. For personal study only.

✦ Synopsis

Co-crystallisation of the imidazo[1,2-a]pyrazine derivative 15 (3-chloro-N-(4-morpholinophenyl)-6-(pyridin-3-yl)imidazo[1,2-a]pyrazin-8-amine) with Aurora-A provided an insight into the interactions of this class of compound with Aurora kinases. This led to the design and synthesis of potent Aurora-A inhibitors demonstrating up to 70-fold selectivity in cell-based Aurora kinase pharmacodynamic biomarker assays.

📜 SIMILAR VOLUMES

Docking and quantitative structure–activ

Docking and quantitative structure–activity relationship studies for imidazo[1,2-a]pyrazines as inhibitors of checkpoint kinase-1

✍ Julio Caballero, Szymon Zilocchi, William Tiznado, Simona Collina 📂 Article 📅 2011 🏛 Springer-Verlag 🌐 English ⚖ 611 KB

Design and evaluation of 3,6-di(hetero)a

Design and evaluation of 3,6-di(hetero)aryl imidazo[1,2-a]pyrazines as inhibitors of checkpoint and other kinases

✍ Thomas P. Matthews; Tatiana McHardy; Suki Klair; Kathy Boxall; Martin Fisher; Mi 📂 Article 📅 2010 🏛 Elsevier Science 🌐 English ⚖ 585 KB

Imidazo[1,2-a]pyridines: A Potent and Se

Imidazo[1,2-a]pyridines: A Potent and Selective Class of Cyclin-Dependent Kinase Inhibitors Identified Through Structure-Based Hybridisation.

✍ Gloria A. Breault; Andrew P. Thomas; Philip J. Jewsbury; et al. et al. 📂 Article 📅 2003 🏛 John Wiley and Sons ⚖ 119 KB 👁 2 views

ChemInform Abstract: Design and Evaluati

ChemInform Abstract: Design and Evaluation of 3,6-Di(hetero)aryl Imidazo[1,2-a]pyrazines as Inhibitors of Checkpoint and Other Kinases.

✍ Thomas P. Matthews; et al. et al. 📂 Article 📅 2010 🏛 John Wiley and Sons ⚖ 29 KB 👁 1 views

Modulation of the Megakaryoblastic Dami

Modulation of the Megakaryoblastic Dami Cell Line Differentiation by Phosphodiesterase Inhibitors and Imidazo[1,2-a]pyrazine Derivatives

✍ Zurbonsen, Katja ;Michel, Alain ;Vittet, Daniel ;Bonnet, Pierre-Antoine ;Chevill 📂 Article 📅 1997 🏛 John Wiley and Sons 🌐 English ⚖ 353 KB

Apoptotic effects of imidazo[1,2-a]pyraz

Apoptotic effects of imidazo[1,2-a]pyrazine derivatives in the human Dami cell line

✍ Katja Zurbonsen; Alain Michel; Pierre-Antoine Bonnet; Leila Gannoun-Zaki; Marie- 📂 Article 📅 1997 🏛 Elsevier Science 🌐 English ⚖ 356 KB