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[(4-Hydroxyl-benzo[4,5]thieno[3,2-c]pyridine-3-carbonyl)-amino]-acetic acid derivatives; HIF prolyl 4-hydroxylase inhibitors as oral erythropoietin secretagogues

2013; Elsevier BV; Volume: 23; Issue: 21 Linguagem: Inglês

10.1016/j.bmcl.2013.08.067

1464-3405

Yong Rae Hong, Hyun Tae Kim, Seung‐Chul Lee, Seonggu Ro, Joong Myung Cho, In Su Kim, Young Hoon Jung,

Metabolomics and Mass Spectrometry Studies

A new series of PHD (HIF prolyl 4-hydroxylase) inhibitors was designed based on the X-ray co-crystal structure of FG-2216. Using a lead generation process, a series of [(4-Hydroxyl-benzo[4,5]thieno[3,2-c]pyridine-3-carbonyl)-amino]-acetic acid derivatives was developed as potent PHD2 inhibitors. This class of compounds also showed the ability to stabilize HIF-α, to stimulate EPO secretion in in vitro studies, and to increase hematocrit, red blood cell count, and hemoglobin levels in an animal efficacy study.