Literature DB >> 18434145

Discovery of a novel and potent series of thieno[3,2-b]pyridine-based inhibitors of c-Met and VEGFR2 tyrosine kinases.

Stephen Claridge1, Franck Raeppel, Marie-Claude Granger, Naomy Bernstein, Oscar Saavedra, Lijie Zhan, David Llewellyn, Amal Wahhab, Robert Deziel, Jubrail Rahil, Normand Beaulieu, Hannah Nguyen, Isabelle Dupont, Annie Barsalou, Carole Beaulieu, Ian Chute, Serge Gravel, Marie-France Robert, Sylvain Lefebvre, Marja Dubay, Roussen Pascal, Jeff Gillespie, Zhiyun Jin, James Wang, Jeffrey M Besterman, A Robert MacLeod, Arkadii Vaisburg.   

Abstract

A series of thieno[3,2-b]pyridine-based inhibitors of c-Met and VEGFR2 tyrosine kinases is described. The compounds demonstrated potency with IC(50) values in the low nanomolar range in vitro while the lead compound also showed in vivo activity against various human tumor xenograft models in mice. Further exploration of this class of compounds is underway.

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Year:  2008        PMID： 18434145     DOI： 10.1016/j.bmcl.2008.04.009

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


  4 in total

1.  Discovery of Anilinopyrimidines as Dual Inhibitors of c-Met and VEGFR-2: Synthesis, SAR, and Cellular Activity.

Authors:  Zhengsheng Zhan; Jing Ai; Qiufeng Liu; Yinchun Ji; Tiantian Chen; Yechun Xu; Meiyu Geng; Wenhu Duan
Journal:  ACS Med Chem Lett       Date:  2014-03-26       Impact factor: 4.345

2.  Phase II Study of Cabozantinib in Patients With Bone Metastasis.

Authors:  Edwin Choy; Gregory M Cote; M Dror Michaelson; Lori Wirth; Justin F Gainor; Alona Muzikansky; Lecia V Sequist; Ryan J Sullivan; Panagiotis M Fidias; Alice Shaw; Rebecca S Heist
Journal:  Oncologist       Date:  2022-07-05       Impact factor: 5.837

3.  1-aryl-3-[4-(thieno[3,2-d]pyrimidin-4-yloxy)phenyl]ureas as VEGFR-2 tyrosine kinase inhibitors: synthesis, biological evaluation, and molecular modelling studies.

Authors:  Pedro Soares; Raquel Costa; Hugo J C Froufe; Ricardo C Calhelha; Daniela Peixoto; Isabel C F R Ferreira; Rui M V Abreu; Raquel Soares; Maria-João R P Queiroz
Journal:  Biomed Res Int       Date:  2013-07-07       Impact factor: 3.411

4.  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
  4 in total

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