Literature DB >> 19111461

Thienopyrimidine-based dual EGFR/ErbB-2 inhibitors.

Tara R Rheault1, Thomas R Caferro, Scott H Dickerson, Kelly H Donaldson, Michael D Gaul, Aaron S Goetz, Robert J Mullin, Octerloney B McDonald, Kimberly G Petrov, David W Rusnak, Lisa M Shewchuk, Glenn M Spehar, Anne T Truesdale, Dana E Vanderwall, Edgar R Wood, David E Uehling.   

Abstract

Two new series of potent and selective dual EGFR/ErbB-2 kinase inhibitors derived from novel thienopyrimidine cores have been identified. Isomeric thienopyrimidine cores were evaluated as isosteres for a 4-anilinoquinazoline core and several analogs containing the thieno[3,2-d]pyrimidine core showed anti-proliferative activity with IC(50) values less than 1 microM against human tumor cells in vitro.

Entities:  

Mesh：

Substances：

Year:  2008        PMID： 19111461     DOI： 10.1016/j.bmcl.2008.12.011

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


  7 in total

1.  Measuring and interpreting the selectivity of protein kinase inhibitors.

Authors:  Lynette A Smyth; Ian Collins
Journal:  J Chem Biol       Date:  2009-06-06

2.  Bichalcophenes: A Concise Synthesis of Formyl Ester- and Cyano Ester-Substituted Bithiophenes, Bifurans, and Furanothiophenes.

Authors:  Abdelbasset A Farahat; Arvind Kumar; Alaa El-Din M Barghash; Fatma E Goda; Hassan M Eisa; David W Boykin
Journal:  J Heterocycl Chem       Date:  2010-01-08       Impact factor: 2.193

Review 3.  A Review on Fused Pyrimidine Systems as EGFR Inhibitors and Their Structure-Activity Relationship.

Authors:  Tanuja T Yadav; Gulam Moin Shaikh; Maushmi S Kumar; Meena Chintamaneni; Mayur Yc
Journal:  Front Chem       Date:  2022-06-13       Impact factor: 5.545

4.  Covalent inhibitors of EGFR family protein kinases induce degradation of human Tribbles 2 (TRIB2) pseudokinase in cancer cells.

Authors:  Daniel M Foulkes; Dominic P Byrne; Wayland Yeung; Safal Shrestha; Fiona P Bailey; Samantha Ferries; Claire E Eyers; Karen Keeshan; Carrow Wells; David H Drewry; William J Zuercher; Natarajan Kannan; Patrick A Eyers
Journal:  Sci Signal       Date:  2018-09-25       Impact factor: 8.192

5.  Substrate binding allosterically relieves autoinhibition of the pseudokinase TRIB1.

Authors:  Sam A Jamieson; Zheng Ruan; Abigail E Burgess; Jack R Curry; Hamish D McMillan; Jodi L Brewster; Anita K Dunbier; Alison D Axtman; Natarajan Kannan; Peter D Mace
Journal:  Sci Signal       Date:  2018-09-25       Impact factor: 8.192

6.  QSAR based model for discriminating EGFR inhibitors and non-inhibitors using Random forest.

Authors:  Harinder Singh; Sandeep Singh; Deepak Singla; Subhash M Agarwal; Gajendra P S Raghava
Journal:  Biol Direct       Date:  2015-03-25       Impact factor: 4.540

7.  Discovery of New Apoptosis-Inducing Agents for Breast Cancer Based on Ethyl 2-Amino-4,5,6,7-Tetra Hydrobenzo[b]Thiophene-3-Carboxylate: Synthesis, In Vitro, and In Vivo Activity Evaluation.

Authors:  Emad M Gad; Mohamed S Nafie; Elsayed H Eltamany; Magdy S A G Hammad; Assem Barakat; Ahmed T A Boraei
Journal:  Molecules       Date:  2020-05-28       Impact factor: 4.411
  7 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.