Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 20, Issue 17, Pages 5169-5180Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2012.07.007
Keywords
Receptor tyrosine kinase; c-Met; 2-Aminopyridine-3-carboxamide
Funding
- National Basic Research Program of China [2009CB940903, 2012CB518000]
- National Natural Science Foundation of China [20721003, 81025017]
- National S&T Major Projects [2012ZX09103-101-072]
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A series of 2-aminopyridine-3-carboxamide derivatives against c-Met were designed and synthesized by employing bioisosteric replacement of heterocyclic moieties with the amide bond. The structure-activity relationship (SAR) at various positions of the scaffold was explored. In this study, a promising compound (S)-24o with a c-Met IC50 of 0.022 mu M was identified. The compound exhibited dose-dependent inhibition of the phosphorylation of c-Met as well as downstream signaling in EBC-1 cells. Furthermore, the interactive binding model of (S)-24o with c-Met was elucidated by virtue of a molecular modeling study. (C) 2012 Elsevier Ltd. All rights reserved.
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