Literature DB >> 16483772

Alkynyl pyrimidines as dual EGFR/ErbB2 kinase inhibitors.

Alex G Waterson1, Kirk L Stevens, Michael J Reno, Yue-Mei Zhang, Eric E Boros, Frederic Bouvier, Abdullah Rastagar, David E Uehling, Scott H Dickerson, Bryan Reep, Octerloney B McDonald, Edgar R Wood, David W Rusnak, Krystal J Alligood, Sharon K Rudolph.   

Abstract

Anilinoalkynylpyrimidines were prepared and evaluated as dual EGFR/ErbB2 kinase inhibitors. A preference was found for substituted phenyl and heteroaromatic rings attached to the alkyne. In addition, the presence of a potential hydrogen bond donor appended to this ring was favored. Selected molecules in the series demonstrated some activity against human tumor cell lines.

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Year:  2006        PMID: 16483772     DOI: 10.1016/j.bmcl.2006.01.111

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


  2 in total

1.  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

2.  Evaluation of the published kinase inhibitor set to identify multiple inhibitors of bacterial ATP-dependent mur ligases.

Authors:  Martina Hrast; Kaja Rožman; Iza Ogris; Veronika Škedelj; Delphine Patin; Matej Sova; Hélène Barreteau; Stanislav Gobec; Simona Golič Grdadolnik; Anamarija Zega
Journal:  J Enzyme Inhib Med Chem       Date:  2019-12       Impact factor: 5.051

  2 in total

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