Literature DB >> 17398093

Imidazole moiety replacements in the 3-(1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one inhibitors of insulin-like growth factor receptor-1 (IGF-1R) to improve cytochrome P450 profile.

Upender Velaparthi1, Peiying Liu, Balu Balasubramanian, Joan Carboni, Ricardo Attar, Marco Gottardis, Aixin Li, Ann Greer, Mary Zoeckler, Mark D Wittman, Dolatrai Vyas.   

Abstract

A series of 3-(1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one inhibitors of insulin-like growth factor receptor-1 (IGF-1R) were examined in which the pendant imidazole moiety was replaced to improve selectivity for IGF-1R inhibition over cytochrome P450 (CYP). Synthesis and SAR of these compounds is presented.

Entities:  

Mesh:

Substances:

Year:  2007        PMID: 17398093     DOI: 10.1016/j.bmcl.2007.03.048

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


  5 in total

1.  Synthesis and in vitro cytotoxic evaluation of novel N-(3,4,5-trimethoxyphenyl)pyridin-2(1H)-one derivatives.

Authors:  Taijie Chen; Yu Luo; Li Sheng; Jia Li; Youhong Hu; Wei Lu
Journal:  Mol Divers       Date:  2013-04-24       Impact factor: 2.943

Review 2.  Inhibition of the insulin-like growth factor-1 receptor (IGF1R) tyrosine kinase as a novel cancer therapy approach.

Authors:  Rongshi Li; Alan Pourpak; Stephan W Morris
Journal:  J Med Chem       Date:  2009-08-27       Impact factor: 7.446

3.  Design and synthesis of a novel tyrosine kinase inhibitor template.

Authors:  P Jake Slavish; Qin Jiang; Xiaoli Cui; Stephan W Morris; Thomas R Webb
Journal:  Bioorg Med Chem       Date:  2009-03-27       Impact factor: 3.641

4.  Lead screening for HIV-1 integrase (IN) inhibited by traditional Chinese medicine.

Authors:  Tzu-Chieh Hung; Wen-Yuan Lee; Kuen-Bao Chen; Yueh-Chiu Chan; Calvin Yu-Chian Chen
Journal:  Biomed Res Int       Date:  2014-06-11       Impact factor: 3.411

5.  In Silico Investigation of Cytochrome P450 2C9 in relation to Aging Using Traditional Chinese Medicine.

Authors:  Tzu-Chieh Hung; Chia-Chen Kuo; Calvin Yu-Chian Chen
Journal:  Evid Based Complement Alternat Med       Date:  2014-05-08       Impact factor: 2.629

  5 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.