Discovery of novel hydroxy-thiazoles as HIF-alpha prolyl hydroxylase inhibitors: SAR, synthesis, and modeling evaluation.

Autor: Tegley CM; Chemistry Research and Discovery, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, USA. ctegley@amgen.com, Viswanadhan VN, Biswas K, Frohn MJ, Peterkin TA, Chang C, Bürli RW, Dao JH, Veith H, Rogers N, Yoder SC, Biddlecome G, Tagari P, Allen JR, Hungate RW
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2008 Jul 15; Vol. 18 (14), pp. 3925-8. Date of Electronic Publication: 2008 Jun 13.
DOI: 10.1016/j.bmcl.2008.06.031
Abstrakt: Inhibition of the PHD2 enzyme has been associated with increased red blood cell levels. From a screening hit, a series of novel hydroxyl-thiazoles were developed as potent PHD2 inhibitors.
Databáze: MEDLINE