Design of novel quinazoline derivatives and related analogues as potent and selective ALK5 inhibitors
Journal Article
·
· Bioorg. Med. Chem. Lett.
Starting from quinazoline 3a, we designed potent and selective ALK5 inhibitors over p38MAP kinase from a rational drug design approach based on co-crystal structures in the human ALK5 kinase domain. The quinazoline 3d exhibited also in vivo activity in an acute rat model of DMN-induced liver fibrosis when administered orally at 5 mg/kg (bid).
- Research Organization:
- Argonne National Laboratory (ANL)
- Sponsoring Organization:
- USDOE
- OSTI ID:
- 1005727
- Journal Information:
- Bioorg. Med. Chem. Lett., Journal Name: Bioorg. Med. Chem. Lett. Journal Issue: (8) ; 04, 2009 Vol. 19; ISSN 0960-894X
- Country of Publication:
- United States
- Language:
- ENGLISH
Similar Records
Identification of quinazoline based inhibitors of IRAK4 for the treatment of inflammation
Novel mutant-selective EGFR kinase inhibitors against EGFR T790M
Pyrazolo-Pyrimidines: A Novel Heterocyclic Scaffold for Potent and Selective p38alpha Inhibitors
Journal Article
·
Thu Jun 01 00:00:00 EDT 2017
· Bioorganic and Medicinal Chemistry Letters
·
OSTI ID:1404982
Novel mutant-selective EGFR kinase inhibitors against EGFR T790M
Journal Article
·
Mon Jan 11 23:00:00 EST 2010
· Nature
·
OSTI ID:1006040
Pyrazolo-Pyrimidines: A Novel Heterocyclic Scaffold for Potent and Selective p38alpha Inhibitors
Journal Article
·
Mon Dec 31 23:00:00 EST 2007
· BioOrganic and Medicinal Chemistry Letters
·
OSTI ID:959850