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Title: Design of novel quinazoline derivatives and related analogues as potent and selective ALK5 inhibitors

Abstract

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).

Authors:
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  1. (
Publication Date:
Research Org.:
Argonne National Lab. (ANL), Argonne, IL (United States)
Sponsoring Org.:
USDOE
OSTI Identifier:
1005727
Resource Type:
Journal Article
Journal Name:
Bioorg. Med. Chem. Lett.
Additional Journal Information:
Journal Volume: 19; Journal Issue: (8) ; 04, 2009; Journal ID: ISSN 0960-894X
Country of Publication:
United States
Language:
ENGLISH
Subject:
59 BASIC BIOLOGICAL SCIENCES; 99 GENERAL AND MISCELLANEOUS//MATHEMATICS, COMPUTING, AND INFORMATION SCIENCE; DESIGN; FIBROSIS; IN VIVO; LIVER; PHOSPHOTRANSFERASES

Citation Formats

Gellibert, F., Fouchet, M.-H., Nguyen, V.-L., Wang, R., Krysa, G., de Gouville, A.-C., Huet, S., Dodic, N., GSKNC), and GSK). Design of novel quinazoline derivatives and related analogues as potent and selective ALK5 inhibitors. United States: N. p., 2009. Web. doi:10.1016/j.bmcl.2009.02.087.
Gellibert, F., Fouchet, M.-H., Nguyen, V.-L., Wang, R., Krysa, G., de Gouville, A.-C., Huet, S., Dodic, N., GSKNC), & GSK). Design of novel quinazoline derivatives and related analogues as potent and selective ALK5 inhibitors. United States. doi:10.1016/j.bmcl.2009.02.087.
Gellibert, F., Fouchet, M.-H., Nguyen, V.-L., Wang, R., Krysa, G., de Gouville, A.-C., Huet, S., Dodic, N., GSKNC), and GSK). Thu . "Design of novel quinazoline derivatives and related analogues as potent and selective ALK5 inhibitors". United States. doi:10.1016/j.bmcl.2009.02.087.
@article{osti_1005727,
title = {Design of novel quinazoline derivatives and related analogues as potent and selective ALK5 inhibitors},
author = {Gellibert, F. and Fouchet, M.-H. and Nguyen, V.-L. and Wang, R. and Krysa, G. and de Gouville, A.-C. and Huet, S. and Dodic, N. and GSKNC) and GSK)},
abstractNote = {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).},
doi = {10.1016/j.bmcl.2009.02.087},
journal = {Bioorg. Med. Chem. Lett.},
issn = {0960-894X},
number = (8) ; 04, 2009,
volume = 19,
place = {United States},
year = {2009},
month = {7}
}