Novel imidazo [1, 2-a] pyridine based inhibitors of the IGF-1 receptor tyrosine kinase: optimization of the aniline

…, CD Jones, FH Jung, I Simpson, J Curwen…

Index: Ducray, Richard; Jones, Clifford D.; Jung, Frederic H.; Simpson, Iain; Curwen, Jon; Pass, Martin Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 16 p. 4702 - 4704

Full Text: HTML

Citation Number: 20

Abstract

Following the discovery of imidazopyridine 1 as a potent IGF-1R tyrosine kinase inhibitor, the aniline part has been modified with the aim to optimize the properties of this series. The structure–activity relationships against IGF-1R kinase activity as well as inhibition of the hERG ion channel are discussed.

~66%

Synthesis and SAR of aminopyrimidines as novel c-Jun N-termi...

[Alam, Mahbub; Beevers, Rebekah E.; Ceska, Tom; Davenport, Richard J.; Dickson, Karen M.; Fortunato, Mara; Gowers, Lewis; Haughan, Alan F.; James, Lynwen A.; Jones, Mark W.; Kinsella, Natasha; Lowe, Christopher; Meissner, Johannes W.G.; Nicolas, Anne-Lise; Perry, Benjamin G.; Phillips, David J.; Pitt, William R.; Platt, Adam; Ratcliffe, Andrew J.; Sharpe, Andrew; Tait, Laura J. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 12 p. 3463 - 3467]

A versatile route to 3-(pyrimidin-4-yl)-imidazo [1, 2-a] pyr...

[Ducray, Richard; Boutron, Pascal; Didelot, Myriam; Germain, Herve; Lach, Franck; Lamorlette, Maryannick; Legriffon, Antoine; Maudet, Mickael; Menard, Morgan; Pasquet, Georges; Renaud, Fabrice; Simpson, Iain; Young, Gail L. Tetrahedron Letters, 2010 , vol. 51, # 36 p. 4755 - 4758]

Imidazo [1, 2-a] pyridines. Part 2: SAR and optimisation of ...

[Byth, Kate F.; Culshaw, Janet D.; Green, Stephen; Oakes, Sandra E.; Thomas, Andrew P. Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 9 p. 2245 - 2248]