Discovery of a 2,4-disubstituted pyrrolo[1,2-f][1,2,4]triazine inhibitor (BMS-754807) of insulin-like growth factor receptor (IGF-1R) kinase in clinical development

  • J Med Chem. 2009 Dec 10;52(23):7360-3. doi: 10.1021/jm900786r.
Mark D Wittman  1 ,  Joan M Carboni ,  Zheng Yang ,  Francis Y Lee ,  Melissa Antman ,  Ricardo Attar ,  Praveen Balimane ,  Chiehying Chang ,  Cliff Chen ,  Lorell Discenza ,  David Frennesson ,  Marco M Gottardis ,  Ann Greer ,  Warren Hurlburt ,  Walter Johnson ,  David R Langley ,  Aixin Li ,  Jianqing Li ,  Peiying Liu ,  Harold Mastalerz ,  Arvind Mathur ,  Krista Menard ,  Karishma Patel ,  John Sack ,  Xiaopeng Sang ,  Mark Saulnier ,  Daniel Smith ,  Kevin Stefanski ,  George Trainor ,  Upender Velaparthi ,  Guifen Zhang ,  Kurt Zimmermann ,  Dolatrai M Vyas
Affiliations
  • 1. Bristol-Myers Squibb Co, Wallingford, Connecticut 06492, USA.
PMID: 19778024 DOI: 10.1021/jm900786r
Abstract

This report describes the biological activity, characterization, and SAR leading to 9d (BMS-754807) a small molecule IGF-1R kinase inhibitor in clinical development.

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