Literature DB >> 12941311

Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 1: identification and optimisation of substituted 4,6-bis anilino pyrimidines.

John F Beattie1, Gloria A Breault, Rebecca P A Ellston, Stephen Green, Philip J Jewsbury, Catherine J Midgley, Russell T Naven, Claire A Minshull, Richard A Pauptit, Julie A Tucker, J Elizabeth Pease.   

Abstract

Using a high-throughput screening campaign, we identified the 4,6-bis anilino pyrimidines as inhibitors of the cyclin-dependent kinase, CDK4. Herein we describe the further chemical modification and use of X-ray crystallography to develop potent and selective in vitro inhibitors of CDK4.

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Year:  2003        PMID： 12941311     DOI： 10.1016/s0960-894x(03)00202-6

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


  13 in total

1.  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

2.  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

3.  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

Review 4.  Current status of PTMs structural databases: applications, limitations and prospects.

Authors:  Alexandre G de Brevern; Joseph Rebehmed
Journal:  Amino Acids       Date:  2022-01-12       Impact factor: 3.520

Review 5.  Selectivity and potency of cyclin-dependent kinase inhibitors.

Authors:  Jayalakshmi Sridhar; Nagaraju Akula; Nagarajan Pattabiraman
Journal:  AAPS J       Date:  2006-03-24       Impact factor: 4.009

6.  Expanding the diversity of allosteric bcr-abl inhibitors.

Authors:  Xianming Deng; Barun Okram; Qiang Ding; Jianming Zhang; Yongmun Choi; Francisco J Adrián; Amy Wojciechowski; Guobao Zhang; Jianwei Che; Badry Bursulaya; Sandra W Cowan-Jacob; Gabriele Rummel; Taebo Sim; Nathanael S Gray
Journal:  J Med Chem       Date:  2010-10-14       Impact factor: 7.446

7.  Crystal structures of the FAK kinase in complex with TAE226 and related bis-anilino pyrimidine inhibitors reveal a helical DFG conformation.

Authors:  Daniel Lietha; Michael J Eck
Journal:  PLoS One       Date:  2008-11-24       Impact factor: 3.240

8.  Analysing the Effect of Mutation on Protein Function and Discovering Potential Inhibitors of CDK4: Molecular Modelling and Dynamics Studies.

Authors:  Nagasundaram N; Hailong Zhu; Jiming Liu; Karthick V; George Priya Doss C; Chiranjib Chakraborty; Luonan Chen
Journal:  PLoS One       Date:  2015-08-07       Impact factor: 3.240

9.  Antitumour potential of BPT: a dual inhibitor of cdk4 and tubulin polymerization.

Authors:  S Mahale; S B Bharate; S Manda; P Joshi; P R Jenkins; R A Vishwakarma; B Chaudhuri
Journal:  Cell Death Dis       Date:  2015-05-07       Impact factor: 8.469

10.  Specific non-local interactions are not necessary for recovering native protein dynamics.

Authors:  Bhaskar Dasgupta; Kota Kasahara; Narutoshi Kamiya; Haruki Nakamura; Akira R Kinjo
Journal:  PLoS One       Date:  2014-03-13       Impact factor: 3.240
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