4deh › Citations

Discovery and optimization of a potent and selective triazolopyridinone series of c-Met inhibitors.

Bode CM, Boezio AA, Albrecht BK, Bellon SF, Berry L, Broome MA, Choquette D, Dussault I, Lewis RT, Lin MH, Rex K, Whittington DA, Yang Y, Harmange JC
Bioorg Med Chem Lett 22 4089-93 (2012)
Related entries: 4deg, 4dei

Cited: 3 times
EuropePMC logo PMID: 22595176

Abstract

Deregulation of the receptor tyrosine kinase c-Met has been implicated in several human cancers and is an attractive target for small molecule drug discovery. Herein, we report the discovery of a structurally diverse series of carbon-linked quinoline triazolopyridinones, which demonstrates nanomolar inhibition of c-Met kinase activity. This novel series of inhibitors exhibits favorable pharmacokinetics as well as potent inhibition of HGF-mediated c-Met phosphorylation in a mouse liver pharmacodynamic model.

Articles - 4deh mentioned but not cited (2)

  1. Data driven polypharmacological drug design for lung cancer: analyses for targeting ALK, MET, and EGFR. Narayanan D, Gani OABSM, Gruber FXE, Engh RA. J Cheminform 9 43 (2017)
  2. Prediction of kinase-inhibitor binding affinity using energetic parameters. Usha S, Selvaraj S. Bioinformation 12 172-181 (2016)


Reviews citing this publication (1)

  1. The Exploration of Chirality for Improved Druggability within the Human Kinome. Saha D, Kharbanda A, Yan W, Lakkaniga NR, Frett B, Li HY. J Med Chem 63 441-469 (2020)


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