Literature DB >> 12270156

Synthesis and kinase inhibitory activity of 3'-(S)-epi-K-252a.

Diane E Gingrich1, Robert L Hudkins.   

Abstract

The 3'-epi diastereomer of K-252a was synthesized with the goal of evaluating the stereochemical requirements of the 3'-sugar alcohol on kinase inhibitory activity. Inverting the 3'-alcohol resulted in a 20 nM inhibitor of VEGFR2 and a 1 nM inhibitor of TrkA tyrosine kinase.

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Year:  2002        PMID: 12270156     DOI: 10.1016/s0960-894x(02)00638-8

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


  2 in total

1.  Lestaurtinib inhibits histone phosphorylation and androgen-dependent gene expression in prostate cancer cells.

Authors:  Jens Köhler; German Erlenkamp; Adrien Eberlin; Tobias Rumpf; Inna Slynko; Eric Metzger; Roland Schüle; Wolfgang Sippl; Manfred Jung
Journal:  PLoS One       Date:  2012-04-20       Impact factor: 3.240

2.  Targeting the JAK/STAT pathway in solid tumors.

Authors:  Zoya Qureshy; Daniel E Johnson; Jennifer R Grandis
Journal:  J Cancer Metastasis Treat       Date:  2020-08-21
  2 in total

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