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

被引：12

作者：

Shaikh, Jahara ^{[1
]}

Patel, Kavitkumar ^{[1
]}

Khan, Tabassum ^{[1
]}

机构：

[1] SVKMS Dr Bhanuben Nanavati Coll Pharm, Dept Pharmaceut Chem & Qual Assurance, Mumbai 56, Maharashtra, India

来源：

MINI-REVIEWS IN MEDICINAL CHEMISTRY | 2022年 / 22卷 / 08期

关键词：

Cyclin-Dependent Kinase (CDK) inhibitor; cell cycle; CDK2; inhibitors; pyrazole derivatives; SAR; anti-cancer agents; X-RAY CRYSTALLOGRAPHY; DINACICLIB SCH 727965; BREAST-CANCER; CELL-CYCLE; CDK INHIBITORS; CDK2-DEPENDENT PHOSPHORYLATION; BIOLOGICAL EVALUATION; MOLECULAR DOCKING; 3-AMINOPYRAZOLE INHIBITORS; THERAPEUTIC TARGETS;

D O I：

10.2174/1389557521666211027104957

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 anti-proliferative 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.

引用

页码：1197 / 1215

页数：19

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