Literature DB >> 12941312

Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 2: identification and optimisation of substituted 2,4-bis anilino pyrimidines.

Gloria A Breault1, Rebecca P A Ellston, Stephen Green, S Russell James, Philip J Jewsbury, Catherine J Midgley, Richard A Pauptit, Claire A Minshull, Julie A Tucker, J Elizabeth Pease.   

Abstract

Through chemical modification and X-ray crystallography we identified the 2,4-bis anilino pyrimidines as potent inhibitors of CDK4. Herein, we describe the optimisation of this series.

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Year:  2003        PMID： 12941312     DOI： 10.1016/s0960-894x(03)00203-8

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


  8 in total

1.  Substantial improvements in large-scale redocking and screening using the novel HYDE scoring function.

Authors:  Nadine Schneider; Sally Hindle; Gudrun Lange; Robert Klein; Jürgen Albrecht; Hans Briem; Kristin Beyer; Holger Claußen; Marcus Gastreich; Christian Lemmen; Matthias Rarey
Journal:  J Comput Aided Mol Des       Date:  2011-12-27       Impact factor: 3.686

2.  Feature-map vectors: a new class of informative descriptors for computational drug discovery.

Authors:  Gregory A Landrum; Julie E Penzotti; Santosh Putta
Journal:  J Comput Aided Mol Des       Date:  2007-01-05       Impact factor: 3.686

3.  The effect of a tightly bound water molecule on scaffold diversity in the computer-aided de novo ligand design of CDK2 inhibitors.

Authors:  Alfonso T García-Sosa; Ricardo L Mancera
Journal:  J Mol Model       Date:  2005-12-23       Impact factor: 1.810

4.  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

5.  Development of o-chlorophenyl substituted pyrimidines as exceptionally potent aurora kinase inhibitors.

Authors:  Matthew P Martin; Yunting Luo; Roberta Pireddu; Hua Yang; Harsukh Gevariya; Harshani R Lawrence; Sevil Ozcan; Jin-Yi Zhu; Robert Kendig; Mercedes Rodriguez; Roy Elias; Jin Q Cheng; Saïd M Sebti; Ernst Schonbrunn; Nicholas J Lawrence
Journal:  J Med Chem       Date:  2012-08-30       Impact factor: 7.446

6.  Novel mutant-selective EGFR kinase inhibitors against EGFR T790M.

Authors:  Wenjun Zhou; Dalia Ercan; Liang Chen; Cai-Hong Yun; Danan Li; Marzia Capelletti; Alexis B Cortot; Lucian Chirieac; Roxana E Iacob; Robert Padera; John R Engen; Kwok-Kin Wong; Michael J Eck; Nathanael S Gray; Pasi A Jänne
Journal:  Nature       Date:  2009-12-24       Impact factor: 49.962

7.  Pd(OAc)2-catalyzed dehydrogenative C-H activation: An expedient synthesis of uracil-annulated β-carbolinones.

Authors:  Biplab Mondal; Somjit Hazra; Tarun K Panda; Brindaban Roy
Journal:  Beilstein J Org Chem       Date:  2015-08-04       Impact factor: 2.883

8.  Antiproliferative Activity of (-)-Isopulegol-based 1,3-Oxazine, 1,3-Thiazine and 2,4-Diaminopyrimidine Derivatives.

Authors:  Fatima Z Bamou; Tam M Le; Bizhar A Tayeb; Seyyed A S Tahaei; Renáta Minorics; István Zupkó; Zsolt Szakonyi
Journal:  ChemistryOpen       Date:  2022-10       Impact factor: 2.630
  8 in total

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