Ontology highlight
ABSTRACT:
SUBMITTER: Hutchings KM
PROVIDER: S-EPMC5395305 | biostudies-literature | 2017 Apr
REPOSITORIES: biostudies-literature
Bioorganic & medicinal chemistry letters 20170310 8
We recently reported the development of a novel inhibitor of Rho-mediated gene transcription (1, CCG-203971) that is efficacious in multiple animal models of acute fibrosis, including scleroderma, when given intraperitoneally. The modest in vivo potency and poor pharmacokinetics (PK) of this lead, however, make it unsuitable for long term efficacy studies. We therefore undertook a systematic medicinal chemistry effort to improve both the metabolic stability and the solubility of 1, resulting in ...[more]