Synthesis, initial SAR and biological evaluation of 1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine derived inhibitors of IkappaB kinase.

Abstract

A new series of tricyclic-based inhibitors of IKK have been derived from an earlier lead compound. The synthesis and structure-activity relationships (SAR) are described. Compound 4k inhibited TNF production in rats stimulated with LPS.

DOI: 10.1016/j.bmcl.2009.03.159

Cite this paper

@article{Kempson2009SynthesisIS, title={Synthesis, initial SAR and biological evaluation of 1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine derived inhibitors of IkappaB kinase.}, author={James Kempson and Junqing Guo and Jagabandhu Das and Robert V Moquin and Steven H Spergel and Scott H. Watterson and Charles M Langevine and Alaric J Dyckman and Mark A. Pattoli and James R Burke and Xiaoxia Yang and Kathleen M. Gillooly and Kim W Mcintyre and Laishun Chen and John H Dodd and Murray Mckinnon and Joel C Barrish and William J. Pitts}, journal={Bioorganic & medicinal chemistry letters}, year={2009}, volume={19 10}, pages={2646-9} }