Literature DB >> 24185375

Synthesis, structure-activity relationship and biological evaluation of 2,4,5-trisubstituted pyrimidine CDK inhibitors as potential anti-tumour agents.

Hao Shao1, Shenhua Shi, David W Foley, Frankie Lam, Abdullah Y Abbas, Xiangrui Liu, Shiliang Huang, Xiangrui Jiang, Nadiah Baharin, Peter M Fischer, Shudong Wang.   

Abstract

A series of 2,4,5-trisubstituted pyrimidines have been synthesised and characterised, which exhibited potent CDK inhibition and anti-proliferative activities. The structure-activity relationship is analysed and a rational for CDK9 selectivity is discussed. Compound 9s, possessing appreciable selectivity for CDK9 over other CDKs, is capable of activating caspase 3, reducing the level of Mcl-1 anti-apoptotic protein, and inducing cancer cell apoptosis. Crown
Copyright © 2013. Published by Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  Anti-cancer drug discovery; CDK9 inhibitors; Inhibitor design; Mcl-1 anti-apoptotic proteins; RNA polymerase II

Mesh：

Substances：

Year:  2013        PMID： 24185375     DOI： 10.1016/j.ejmech.2013.08.052

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN： 0223-5234            Impact factor:   6.514


  6 in total

1.  Discovery of CDK5 Inhibitors through Structure-Guided Approach.

Authors:  Nishat Z Khair; Jimma L Lenjisa; Solomon Tadesse; Malika Kumarasiri; Sunita K C Basnet; Laychiluh B Mekonnen; Manjun Li; Sarah Diab; Matthew J Sykes; Hugo Albrecht; Robert Milne; Shudong Wang
Journal:  ACS Med Chem Lett       Date:  2019-03-20       Impact factor: 4.345

Review 2.  CDK9 inhibitors in cancer research.

Authors:  Zhi Huang; Tianqi Wang; Cheng Wang; Yan Fan
Journal:  RSC Med Chem       Date:  2022-04-20

Review 3.  Overview of CDK9 as a target in cancer research.

Authors:  Fatima Morales; Antonio Giordano
Journal:  Cell Cycle       Date:  2016       Impact factor: 4.534

4.  Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.

Authors:  Yogesh A Sonawane; Margaret A Taylor; John Victor Napoleon; Sandeep Rana; Jacob I Contreras; Amarnath Natarajan
Journal:  J Med Chem       Date:  2016-06-03       Impact factor: 7.446

5.  Design, synthesis, and anti-cancer evaluation of new pyrido[2,3-d]pyrimidin-4(3H)-one derivatives as potential EGFRWT and EGFRT790M inhibitors and apoptosis inducers.

Authors:  Heba S A Elzahabi; Eman S Nossier; Rania A Alasfoury; May El-Manawaty; Sara M Sayed; Eslam B Elkaeed; Ahmed M Metwaly; Mohamed Hagras; Ibrahim H Eissa
Journal:  J Enzyme Inhib Med Chem       Date:  2022-12       Impact factor: 5.756

Review 6.  Therapeutic potential of heterocyclic pyrimidine scaffolds.

Authors:  Sanjiv Kumar; Balasubramanian Narasimhan
Journal:  Chem Cent J       Date:  2018-04-04       Impact factor: 4.215
  6 in total

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