Hit-to-lead studies: the discovery of potent, orally active, thiophenecarboxamide IKK-2 inhibitors

  • Bioorg Med Chem Lett. 2004 Jun 7;14(11):2817-22. doi: 10.1016/j.bmcl.2004.03.058.
Andrew Baxter  1 ,  Steve Brough ,  Anne Cooper ,  Eike Floettmann ,  Steve Foster ,  Christine Harding ,  Jason Kettle ,  Tom McInally ,  Craig Martin ,  Michelle Mobbs ,  Maurice Needham ,  Pete Newham ,  Stuart Paine ,  Steve St-Gallay ,  Sylvia Salter ,  John Unitt ,  Yafeng Xue
Affiliations
  • 1. AstraZeneca R&D Charnwood, Bakewell Road, Loughborough LE11 5RH, UK. [email protected]
PMID: 15125939 DOI: 10.1016/j.bmcl.2004.03.058
Abstract

A hit-to-lead optimisation programme was carried out on the thiophenecarboxamide high throughput screening hits 1 and 2 resulting in the discovery of the potent and orally bioavailable IKK-2 inhibitor 22.

Products