Literature DB >> 19778024

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.

Mark D Wittman1, 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.   

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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Year:  2009        PMID： 19778024     DOI： 10.1021/jm900786r

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  25 in total

1.  Synthesis of aryl-heteroaryl ureas (AHUs) based on 4-aminoquinoline and their evaluation against the insulin-like growth factor receptor (IGF-1R).

Authors:  William Engen; Terrence E O'Brien; Brendan Kelly; Jacinda Do; Liezel Rillera; Lance K Stapleton; Jack F Youngren; Marc O Anderson
Journal:  Bioorg Med Chem       Date:  2010-06-25       Impact factor: 3.641

Review 2.  Insulin receptor (IR) and insulin-like growth factor receptor 1 (IGF-1R) signaling systems: novel treatment strategies for cancer.

Authors:  Pushpendra Singh; Jimi Marin Alex; Felix Bast
Journal:  Med Oncol       Date:  2013-12-14       Impact factor: 3.064

3.  Drug efflux by breast cancer resistance protein is a mechanism of resistance to the benzimidazole insulin-like growth factor receptor/insulin receptor inhibitor, BMS-536924.

Authors:  Xiaonan Hou; Fei Huang; Joan M Carboni; Karen Flatten; Yan W Asmann; Cynthia Ten Eyck; Takeo Nakanishi; Jennifer D Tibodeau; Douglas D Ross; Marco M Gottardis; Charles Erlichman; Scott H Kaufmann; Paul Haluska
Journal:  Mol Cancer Ther       Date:  2011-01       Impact factor: 6.261

4.  An efficient and facile synthesis of new tetracyclic fused pyrazolo[4,3-c][1,2,4]triazino[4,5-a]quinolin-4(5H)-ones.

Authors:  Mohsen A-M Gomaa; Huda A Ali
Journal:  Mol Divers       Date:  2018-07-03       Impact factor: 2.943

5.  Targeting the IGF1R/PI3K/AKT Pathway Sensitizes Ewing Sarcoma to BET Bromodomain Inhibitors.

Authors:  Sudan N Loganathan; Nan Tang; Albert E Holler; Nenghui Wang; Jialiang Wang
Journal:  Mol Cancer Ther       Date:  2019-03-29       Impact factor: 6.261

6.  In vivo evaluation of IGF1R/IR PET ligand [18F]BMS-754807 in rodents.

Authors:  Jaya Prabhakaran; Stephen L Dewey; Richard McClure; Norman R Simpson; Mohammed N Tantawy; J John Mann; Wellington Pham; J S Dileep Kumar
Journal:  Bioorg Med Chem Lett       Date:  2017-01-07       Impact factor: 2.823

7.  Discovery of a potent inhibitor of anaplastic lymphoma kinase with in vivo antitumor activity.

Authors:  Gregory R Ott; Rabindranath Tripathy; Mangeng Cheng; Robert McHugh; Andrew V Anzalone; Ted L Underiner; Matthew A Curry; Matthew R Quail; Lihui Lu; Weihua Wan; Thelma S Angeles; Mark S Albom; Lisa D Aimone; Mark A Ator; Bruce A Ruggeri; Bruce D Dorsey
Journal:  ACS Med Chem Lett       Date:  2010-09-01       Impact factor: 4.345

8.  Serine phosphorylation of the insulin-like growth factor I (IGF-1) receptor C-terminal tail restrains kinase activity and cell growth.

Authors:  Geraldine M Kelly; Deirdre A Buckley; Patrick A Kiely; David R Adams; Rosemary O'Connor
Journal:  J Biol Chem       Date:  2012-06-08       Impact factor: 5.157

Review 9.  Targeting insulin-like growth factor-I and insulin-like growth factor-binding protein-3 signaling pathways. A novel therapeutic approach for asthma.

Authors:  Hyun Lee; So Ri Kim; Youngman Oh; Seong Ho Cho; Robert P Schleimer; Yong Chul Lee
Journal:  Am J Respir Cell Mol Biol       Date:  2014-04       Impact factor: 6.914

10.  Insulin-like growth factor 1 receptor stabilizes the ETV6-NTRK3 chimeric oncoprotein by blocking its KPC1/Rnf123-mediated proteasomal degradation.

Authors:  Cristina E Tognon; Bo Rafn; Naniye Malli Cetinbas; Takumi Kamura; Genny Trigo; Barak Rotblat; Fumihiko Okumura; Masaki Matsumoto; Christine Chow; Monika Davare; Michael Pollak; Thibault Mayor; Poul H Sorensen
Journal:  J Biol Chem       Date:  2018-06-14       Impact factor: 5.157
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