Literature DB >> 12668002

Discovery and SAR of novel Naphthyridines as potent inhibitors of spleen tyrosine kinase (SYK).

Charles L Cywin1, Bao-Ping Zhao, Daniel W McNeil, Matt Hrapchak, Anthony S Prokopowicz, Daniel R Goldberg, Tina M Morwick, Amy Gao, Scott Jakes, Mohammed Kashem, Ronald L Magolda, Richard M Soll, Mark R Player, Mark A Bobko, James Rinker, Renee L DesJarlais, Michael P Winters.   

Abstract

The discovery of novel 5,7-disubstituted[1,6]naphthyridines as potent inhibitors of Spleen Tyrosine Kinase (SYK) is discussed. The SAR reveals the necessity for a 7-aryl group with preference towards para substitution and that this in combination with 5-aminoalkylamino substituents further improved the potency of the compounds. The initial SAR as well as a survey of the other positions is discussed in detail.

Entities:  

Mesh:

Substances:

Year:  2003        PMID: 12668002     DOI: 10.1016/s0960-894x(03)00163-x

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


  5 in total

1.  Discovery of Lanraplenib (GS-9876): A Once-Daily Spleen Tyrosine Kinase Inhibitor for Autoimmune Diseases.

Authors:  Peter Blomgren; Jayaraman Chandrasekhar; Julie A Di Paolo; Wanchi Fung; Guoju Geng; Carmen Ip; Randall Jones; Jeffrey E Kropf; Eric B Lansdon; Seung Lee; Jennifer R Lo; Scott A Mitchell; Bernard Murray; Chris Pohlmeyer; Aaron Schmitt; Kimberly Suekawa-Pirrone; Sarah Wise; Jin-Ming Xiong; Jianjun Xu; Helen Yu; Zhongdong Zhao; Kevin S Currie
Journal:  ACS Med Chem Lett       Date:  2020-02-12       Impact factor: 4.345

Review 2.  Synthesis and Anticancer Properties of Functionalized 1,6-Naphthyridines.

Authors:  Mallu Lavanya; Chong Lin; Jincheng Mao; Dhakshanamurthy Thirumalai; Sreenath Reddy Aabaka; Xiaojiang Yang; Jinhua Mao; Zhiyu Huang; Jinzhou Zhao
Journal:  Top Curr Chem (Cham)       Date:  2021-02-24

3.  Characterizing the structure-activity relationships of natural products, tanshinones, reveals their mode of action in inhibiting spleen tyrosine kinase.

Authors:  Min-Che Tung; Keng-Chang Tsai; Kit-Man Fung; Ming-Jaw Don; Tien-Sheng Tseng
Journal:  RSC Adv       Date:  2021-01-14       Impact factor: 3.361

4.  Applying ligands profiling using multiple extended electron distribution based field templates and feature trees similarity searching in the discovery of new generation of urea-based antineoplastic kinase inhibitors.

Authors:  Eman M Dokla; Amr H Mahmoud; Mohamed S A Elsayed; Ahmed H El-Khatib; Michael W Linscheid; Khaled A Abouzid
Journal:  PLoS One       Date:  2012-11-20       Impact factor: 3.240

5.  Kinase inhibitors for the treatment of inflammatory and autoimmune disorders.

Authors:  Shripad S Bhagwat
Journal:  Purinergic Signal       Date:  2008-06-21       Impact factor: 3.765

  5 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.