Literature DB >> 16242328

Synthesis and biological evaluation of 3-ethylidene-1,3-dihydro-indol-2-ones as novel checkpoint 1 inhibitors.

Nan-Horng Lin1, Ping Xia, Peter Kovar, Chang Park, Zehan Chen, Haiying Zhang, Saul H Rosenberg, Hing L Sham.   

Abstract

Chk1 inhibitors have emerged as a novel class of neoplastic agents for abrogating the G2 DNA damage checkpoint arrest. Analogs of the Chk1 inhibitor, 3-ethylidene-1,3-dihydro-indol-2-one, were synthesized and tested in vitro for their inhibitory activities. The most promising compound identified from this series is analog 28, which possesses potent enzymatic and cellular activities.

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Year:  2005        PMID: 16242328     DOI: 10.1016/j.bmcl.2005.09.064

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


  4 in total

1.  Discovery of novel checkpoint kinase 1 inhibitors by virtual screening based on multiple crystal structures.

Authors:  Yan Li; Dong Joon Kim; Weiya Ma; Ronald A Lubet; Ann M Bode; Zigang Dong
Journal:  J Chem Inf Model       Date:  2011-10-12       Impact factor: 4.956

2.  A myosin V inhibitor based on privileged chemical scaffolds.

Authors:  Kabirul Islam; Harvey F Chin; Adrian O Olivares; Lauren P Saunders; Enrique M De La Cruz; Tarun M Kapoor
Journal:  Angew Chem Int Ed Engl       Date:  2010-11-02       Impact factor: 15.336

3.  Structure-based and shape-complemented pharmacophore modeling for the discovery of novel checkpoint kinase 1 inhibitors.

Authors:  Xiu-Mei Chen; Tao Lu; Shuai Lu; Hui-Fang Li; Hao-Liang Yuan; Ting Ran; Hai-Chun Liu; Ya-Dong Chen
Journal:  J Mol Model       Date:  2009-12-18       Impact factor: 1.810

4.  CCT244747 is a novel potent and selective CHK1 inhibitor with oral efficacy alone and in combination with genotoxic anticancer drugs.

Authors:  Mike I Walton; Paul D Eve; Angela Hayes; Melanie R Valenti; Alexis K De Haven Brandon; Gary Box; Albert Hallsworth; Elizabeth L Smith; Kathy J Boxall; Michael Lainchbury; Thomas P Matthews; Yann Jamin; Simon P Robinson; G Wynne Aherne; John C Reader; Louis Chesler; Florence I Raynaud; Suzanne A Eccles; Ian Collins; Michelle D Garrett
Journal:  Clin Cancer Res       Date:  2012-08-28       Impact factor: 12.531

  4 in total

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