Literature DB >> 14684289

Design and SAR of thienopyrimidine and thienopyridine inhibitors of VEGFR-2 kinase activity.

Michael J Munchhof1, Jean S Beebe, Jeffery M Casavant, Beth A Cooper, Jonathan L Doty, R Carla Higdon, Stephen M Hillerman, Catherine I Soderstrom, Elisabeth A Knauth, Matthew A Marx, Ann Marie K Rossi, Susan B Sobolov, Jianmin Sun.   

Abstract

Novel classes of thienopyrimidines and thienopyridines have been identified as potent inhibitors of VEGFR-2 kinase. The synthesis and SAR of these compounds is presented, along with successful efforts to diminish EGFR activity present in the lead series.

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Year:  2004        PMID: 14684289     DOI: 10.1016/j.bmcl.2003.10.030

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


  5 in total

1.  Antiproliferative activities of halogenated thieno[3,2-d]pyrimidines.

Authors:  Kartik W Temburnikar; Sarah C Zimmermann; Nathaniel T Kim; Christina R Ross; Christopher Gelbmann; Christine E Salomon; Gerald M Wilson; Jan Balzarini; Katherine L Seley-Radtke
Journal:  Bioorg Med Chem       Date:  2014-03-03       Impact factor: 3.641

2.  In Vitro Anticancer Activity Screening of Novel Fused Thiophene Derivatives as VEGFR-2/AKT Dual Inhibitors and Apoptosis Inducers.

Authors:  Rana M Abdelnaby; Afaf A El-Malah; Rasha R FakhrEldeen; Marwa M Saeed; Rania I Nadeem; Nancy S Younis; Hanaa M Abdel-Rahman; Nehad M El-Dydamony
Journal:  Pharmaceuticals (Basel)       Date:  2022-06-02

3.  Aminodi(hetero)arylamines in the thieno[3,2-b]pyridine series: synthesis, effects in human tumor cells growth, cell cycle analysis, apoptosis and evaluation of toxicity using non-tumor cells.

Authors:  Ricardo C Calhelha; Isabel C F R Ferreira; Daniela Peixoto; Rui M V Abreu; Luís A Vale-Silva; Eugénia Pinto; Raquel T Lima; M Inês Alvelos; M Helena Vasconcelos; Maria-João R P Queiroz
Journal:  Molecules       Date:  2012-03-28       Impact factor: 4.411

4.  Synthesis of Some 4,5-Dihydrothieno[3,2-e][1,2,4]Triazolo[4,3-a] Pyrimi-dine-2-Carboxamides as Anti-Inflammatory and Analgesic Agents.

Authors:  Omaima G Shaaban; Ola H Rizk; Aida E Bayad; Ibrahim M El-Ashmawy
Journal:  Open Med Chem J       Date:  2013-11-29

5.  Synthesis of Novel Methyl 3-(hetero)arylthieno[3,2-b]pyridine-2-carboxylates and Antitumor Activity Evaluation: Studies In Vitro and In Ovo Grafts of Chick Chorioallantoic Membrane (CAM) with a Triple Negative Breast Cancer Cell Line.

Authors:  Bruna R Silva; Rita Rebelo; Juliana M Rodrigues; Cristina P R Xavier; M Helena Vasconcelos; Maria-João R P Queiroz
Journal:  Molecules       Date:  2021-03-13       Impact factor: 4.411

  5 in total

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