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

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

Bioorganic & medicinal chemistry letters (2004-05-06)

Andrew Baxter, 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

PMID15125939

摘要

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.