Literature DB >> 21414779

Discovery of 2,4-bis-arylamino-1,3-pyrimidines as insulin-like growth factor-1 receptor (IGF-1R) inhibitors.

John L Buchanan1, John R Newcomb, David P Carney, Stuart C Chaffee, Lilly Chai, Rod Cupples, Linda F Epstein, Paul Gallant, Yan Gu, Jean-Christophe Harmange, Kathy Hodge, Brett E Houk, Xin Huang, Janan Jona, Smriti Joseph, H Toni Jun, Rakesh Kumar, Chun Li, John Lu, Tom Menges, Michael J Morrison, Perry M Novak, Simon van der Plas, Robert Radinsky, Paul E Rose, Satin Sawant, Ji-Rong Sun, Sekhar Surapaneni, Susan M Turci, Keyang Xu, Evelyn Yanez, Huilin Zhao, Xiaotian Zhu.   

Abstract

The insulin-like growth factor-1 receptor (IGF-1R) plays an important role in the regulation of cell growth and differentiation, and in protection from apoptosis. IGF-1R has been shown to be an appealing target for the treatment of human cancer. Herein, we report the synthesis, structure-activity relationships (SAR), X-ray cocrystal structure and in vivo tumor study results for a series of 2,4-bis-arylamino-1,3-pyrimidines.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID: 21414779     DOI: 10.1016/j.bmcl.2011.02.075

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  7 in total

1.  Molecular biomarkers in the decision of treatment of cervical carcinoma patients.

Authors:  A Valenciano; L A Henríquez-Hernández; M Lloret; B Pinar; P C Lara
Journal:  Clin Transl Oncol       Date:  2013-02-22       Impact factor: 3.405

2.  Role of IGF-1 receptor in radiation response.

Authors:  Almudena Valenciano; Luis Alberto Henríquez-Hernández; Mercedes Moreno; Marta Lloret; Pedro Carlos Lara
Journal:  Transl Oncol       Date:  2012-02-01       Impact factor: 4.243

3.  A highly selective dual insulin receptor (IR)/insulin-like growth factor 1 receptor (IGF-1R) inhibitor derived from an extracellular signal-regulated kinase (ERK) inhibitor.

Authors:  Theonie Anastassiadis; Krisna C Duong-Ly; Sean W Deacon; Alec Lafontant; Haiching Ma; Karthik Devarajan; Roland L Dunbrack; Jinhua Wu; Jeffrey R Peterson
Journal:  J Biol Chem       Date:  2013-08-09       Impact factor: 5.157

Review 4.  Modulation of insulin-like growth factor-1 receptor and its signaling network for the treatment of cancer: current status and future perspectives.

Authors:  Meizhong Jin; Elizabeth Buck; Mark J Mulvihill
Journal:  Oncol Rev       Date:  2013-04-22

5.  Design, Synthesis, and Biological Evaluation of Proteolysis Targeting Chimeras (PROTACs) for the Dual Degradation of IGF-1R and Src.

Authors:  Sudhakar Manda; Na Keum Lee; Dong-Chan Oh; Jeeyeon Lee
Journal:  Molecules       Date:  2020-04-23       Impact factor: 4.411

6.  Regulatory spine RS3 residue of protein kinases: a lipophilic bystander or a decisive element in the small-molecule kinase inhibitor binding?

Authors:  Ekaterina Shevchenko; Tatu Pantsar
Journal:  Biochem Soc Trans       Date:  2022-02-28       Impact factor: 4.919

7.  Development of a 4-aminopyrazolo[3,4-d]pyrimidine-based dual IGF1R/Src inhibitor as a novel anticancer agent with minimal toxicity.

Authors:  Ho Jin Lee; Phuong Chi Pham; Seung Yeob Hyun; Byungyeob Baek; Byungjin Kim; Yunha Kim; Hye-Young Min; Jeeyeon Lee; Ho-Young Lee
Journal:  Mol Cancer       Date:  2018-02-19       Impact factor: 27.401

  7 in total

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