skip to main content
OSTI.GOV title logo U.S. Department of Energy
Office of Scientific and Technical Information

Title: Discovery of orally active pyrrolopyridine- and aminopyridine-based Met kinase inhibitors

Abstract

A series of acylurea analogs derived from pyrrolopyridine and aminopyridine scaffolds were identified as potent inhibitors of Met kinase activity. The SAR at various positions of the two kinase scaffolds was investigated. These studies led to the discovery of compounds 3b and 20b, which demonstrated favorable pharmacokinetic properties in mice and significant antitumor activity in a human gastric carcinoma xenograft model.

Authors:
; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ;  [1]
  1. BMS
Publication Date:
Research Org.:
Argonne National Lab. (ANL), Argonne, IL (United States). Advanced Photon Source (APS)
Sponsoring Org.:
USDOE
OSTI Identifier:
1006818
Resource Type:
Journal Article
Journal Name:
Bioorg. Med. Chem. Lett.
Additional Journal Information:
Journal Volume: 18; Journal Issue: (11) ; 06, 2008; Journal ID: ISSN 0960-894X
Country of Publication:
United States
Language:
ENGLISH
Subject:
59 BASIC BIOLOGICAL SCIENCES; 60 APPLIED LIFE SCIENCES; CARCINOMAS; MICE; PHOSPHOTRANSFERASES

Citation Formats

Cai, Zhen-Wei, Wei, Donna, Schroeder, Gretchen M, Cornelius, Lyndon A.M., Kim, Kyoung, Chen, Xiao-Tao, Schmidt, Robert J, Williams, David K, Tokarski, John S, An, Yongmi, Sack, John S, Manne, Veeraswamy, Kamath, Amrita, Zhang, Yueping, Marathe, Punit, Hunt, John T, Lombardo, Louis J, Fargnoli, Joseph, and Borzilleri, Robert M. Discovery of orally active pyrrolopyridine- and aminopyridine-based Met kinase inhibitors. United States: N. p., 2008. Web. doi:10.1016/j.bmcl.2008.04.047.
Cai, Zhen-Wei, Wei, Donna, Schroeder, Gretchen M, Cornelius, Lyndon A.M., Kim, Kyoung, Chen, Xiao-Tao, Schmidt, Robert J, Williams, David K, Tokarski, John S, An, Yongmi, Sack, John S, Manne, Veeraswamy, Kamath, Amrita, Zhang, Yueping, Marathe, Punit, Hunt, John T, Lombardo, Louis J, Fargnoli, Joseph, & Borzilleri, Robert M. Discovery of orally active pyrrolopyridine- and aminopyridine-based Met kinase inhibitors. United States. https://doi.org/10.1016/j.bmcl.2008.04.047
Cai, Zhen-Wei, Wei, Donna, Schroeder, Gretchen M, Cornelius, Lyndon A.M., Kim, Kyoung, Chen, Xiao-Tao, Schmidt, Robert J, Williams, David K, Tokarski, John S, An, Yongmi, Sack, John S, Manne, Veeraswamy, Kamath, Amrita, Zhang, Yueping, Marathe, Punit, Hunt, John T, Lombardo, Louis J, Fargnoli, Joseph, and Borzilleri, Robert M. 2008. "Discovery of orally active pyrrolopyridine- and aminopyridine-based Met kinase inhibitors". United States. https://doi.org/10.1016/j.bmcl.2008.04.047.
@article{osti_1006818,
title = {Discovery of orally active pyrrolopyridine- and aminopyridine-based Met kinase inhibitors},
author = {Cai, Zhen-Wei and Wei, Donna and Schroeder, Gretchen M and Cornelius, Lyndon A.M. and Kim, Kyoung and Chen, Xiao-Tao and Schmidt, Robert J and Williams, David K and Tokarski, John S and An, Yongmi and Sack, John S and Manne, Veeraswamy and Kamath, Amrita and Zhang, Yueping and Marathe, Punit and Hunt, John T and Lombardo, Louis J and Fargnoli, Joseph and Borzilleri, Robert M},
abstractNote = {A series of acylurea analogs derived from pyrrolopyridine and aminopyridine scaffolds were identified as potent inhibitors of Met kinase activity. The SAR at various positions of the two kinase scaffolds was investigated. These studies led to the discovery of compounds 3b and 20b, which demonstrated favorable pharmacokinetic properties in mice and significant antitumor activity in a human gastric carcinoma xenograft model.},
doi = {10.1016/j.bmcl.2008.04.047},
url = {https://www.osti.gov/biblio/1006818}, journal = {Bioorg. Med. Chem. Lett.},
issn = {0960-894X},
number = (11) ; 06, 2008,
volume = 18,
place = {United States},
year = {Wed Sep 10 00:00:00 EDT 2008},
month = {Wed Sep 10 00:00:00 EDT 2008}
}