Literature DB >> 34711160

Advances in Pyrazole Based Scaffold as Cyclin-dependent Kinase 2 Inhibitors for the Treatment of Cancer.

Jahara Shaikh1, Kavitkumar Patel1, Tabassum Khan1.   

Abstract

The transformation of a normal cell into a tumor cell is one of the initial steps in cell cycle deregulation. The cell cycle is regulated by cyclin-dependent kinases (CDKs) that belong to the protein kinase family. CDK2 is an enchanting target for specific genotype tumors since cyclin E is selective for CDK2 and the deregulation of specific cancer types. Thus, CDKs inhibitor, specifically CDK2/cyclin A-E, has the potential to be a valid cancer target as per the currently undergoing clinical trials. Most of the pyrazole scaffolds have shown selectivity and potency for CDK2 inhibitors. This review aims at examining pyrazole and pyrazole fused with other heterocyclic rings for antiproliferative activity. Based on the in vitro and molecular docking studies, the most potent analogues for CDK2 inhibition are exhibited by IC50 value. Moreover, the review emphasizes the various lead analogs of pyrazole hybrids which can be very potent and selective for anti-cancer drugs. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.

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Keywords:  CDK2 inhibitors; Cyclin-Dependent Kinase (CDK) inhibitor; SAR; anti-cancer agents; cell cycle; pyrazole derivatives

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Year:  2022        PMID: 34711160     DOI: 10.2174/1389557521666211027104957

Source DB:  PubMed          Journal:  Mini Rev Med Chem        ISSN: 1389-5575            Impact factor:   3.862


  1 in total

1.  Selective Cyclin-Dependent Kinase Inhibitors and Their Application in Cancer Therapy.

Authors:  Robert B Kargbo
Journal:  ACS Med Chem Lett       Date:  2022-09-20       Impact factor: 4.632

  1 in total

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