Literature DB >> 18547806

Discovery of a novel class of 2-ureido thiophene carboxamide checkpoint kinase inhibitors.

James W Janetka1, Lynsie Almeida, Susan Ashwell, Patrick J Brassil, Kevin Daly, Chun Deng, Thomas Gero, Roberta E Glynn, Candice L Horn, Stephanos Ioannidis, Paul Lyne, Nicholas J Newcombe, Vibha B Oza, Martin Pass, Stephanie K Springer, Mei Su, Dorin Toader, Melissa M Vasbinder, Dingwei Yu, Yan Yu, Sonya D Zabludoff.   

Abstract

Checkpoint kinase-1 (Chk1, CHEK1) is a Ser/Thr protein kinase that mediates the cellular response to DNA-damage. A novel class of 2-ureido thiophene carboxamide urea (TCU) Chk1 inhibitors is described. Inhibitors in this chemotype were optimized for cellular potency and selectivity over Cdk1.

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Year:  2008        PMID： 18547806     DOI： 10.1016/j.bmcl.2008.05.016

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


  7 in total

1.  Lead optimization studies on FimH antagonists: discovery of potent and orally bioavailable ortho-substituted biphenyl mannosides.

Authors:  Zhenfu Han; Jerome S Pinkner; Bradley Ford; Erik Chorell; Jan M Crowley; Corinne K Cusumano; Scott Campbell; Jeffrey P Henderson; Scott J Hultgren; James W Janetka
Journal:  J Med Chem       Date:  2012-04-13       Impact factor: 7.446

2.  Structural requirements of pyrimidine, thienopyridine and ureido thiophene carboxamide-based inhibitors of the checkpoint kinase 1: QSAR, docking, molecular dynamics analysis.

Authors:  Fangfang Wang; Zhi Ma; Yan Li; Jinan Wang; Yonghua Wang
Journal:  J Mol Model       Date:  2012-01-15       Impact factor: 1.810

3.  Checkpoint kinase 1 prevents cell cycle exit linked to terminal cell differentiation.

Authors:  Zakir Ullah; Christelle de Renty; Melvin L DePamphilis
Journal:  Mol Cell Biol       Date:  2011-07-26       Impact factor: 4.272

Review 4.  Structure-based design, discovery and development of checkpoint kinase inhibitors as potential anticancer therapies.

Authors:  Thomas P Matthews; Alan M Jones; Ian Collins
Journal:  Expert Opin Drug Discov       Date:  2013-04-18       Impact factor: 6.098

5.  Effects of selective checkpoint kinase 1 inhibition on cytarabine cytotoxicity in acute myelogenous leukemia cells in vitro.

Authors:  Erin L Schenk; Brian D Koh; Karen S Flatten; Kevin L Peterson; David Parry; Allan D Hess; B Douglas Smith; Judith E Karp; Larry M Karnitz; Scott H Kaufmann
Journal:  Clin Cancer Res       Date:  2012-08-06       Impact factor: 12.531

6.  Synthesis and structure-activity relationships of 2-amino-3-carboxy-4-phenylthiophenes as novel atypical protein kinase C inhibitors.

Authors:  Paul M Titchenell; H D Showalter; Jean-François Pons; Alistair J Barber; Yafei Jin; David A Antonetti
Journal:  Bioorg Med Chem Lett       Date:  2013-03-13       Impact factor: 2.823

Review 7.  Safeguarding genome integrity: the checkpoint kinases ATR, CHK1 and WEE1 restrain CDK activity during normal DNA replication.

Authors:  Claus Storgaard Sørensen; Randi G Syljuåsen
Journal:  Nucleic Acids Res       Date:  2011-09-21       Impact factor: 16.971
  7 in total

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