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

Mini Rev Med Chem

Department of Pharmaceutical Chemistry & Quality Assurance, SVKM'S Dr. Bhanuben Nanavati College of Pharmacy, Vile Parle (W), Mumbai 56, India.

Published: June 2022

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 IC value. Moreover, the review emphasizes the various lead analogs of pyrazole hybrids which can be very potent and selective for anti-cancer drugs.

Download full-text PDF

Source
http://dx.doi.org/10.2174/1389557521666211027104957DOI Listing

Publication Analysis

Top Keywords

cell cycle
8
advances pyrazole
4
pyrazole based
4
based scaffold
4
scaffold cyclin-dependent
4
cyclin-dependent kinase
4
kinase inhibitors
4
inhibitors treatment
4
treatment cancer
4
cancer transformation
4

Similar Publications

Aging is accompanied by a decline in neovascularization potential and increased susceptibility to ischemic injury. Here, we confirm the age-related impaired neovascularization following ischemic leg injury and impaired angiogenesis. The age-related deficits in angiogenesis arose primarily from diminished EC proliferation capacity, but not migration or VEGF sensitivity.

View Article and Find Full Text PDF

Background: Chronic kidney disease (CKD) is a progressive condition that arises from diverse etiological factors, resulting in structural alterations and functional impairment of the kidneys. We aimed to establish the Anoikis-related gene signature in CKD by bioinformatics analysis.

Methods: We retrieved 3 datasets from the Gene Expression Omnibus (GEO) database to obtain differentially expressed genes (DEGs), followed by Gene Ontology (GO), Kyoto Encyclopedia of Genes and Genomes (KEGG) analysis, Gene Set Enrichment Analysis (GSEA) and Gene Set Variation Analysis (GSVA) of them, which were intersected with Anoikis-related genes (ARGs) to derive Anoikis-related differentially expressed genes (ARDEGs).

View Article and Find Full Text PDF

Purpose: A promising feature of marine sponges is the potential anticancer efficacy of their secondary metabolites. The objective of this study was to explore the anticancer activities of compounds from the fungal symbiont of on breast cancer cells.

Methods: In the present research, , an endophytic fungal strain derived from the marine sponge was successfully isolated and characterized.

View Article and Find Full Text PDF

Unlabelled: High expression of Fascin-1 involves high metastasis, high recurrence, and poor prognosis of cancers. However, the related regulatory mechanism in hepatocellular carcinoma (HCC) remains elusive. In this study, Fascin-1 was highly expressed in HCC tissues and cell lines.

View Article and Find Full Text PDF

Improving mammary gland epithelial cells proliferation through nutrition is an important approach for enhancing sow milk production and piglet growth. An intermediate metabolite of valine, 3-hydroxyisobutyrate (3-HIB), regulates cellular lipid metabolism. In the present study, we investigated the effects of 3-HIB on porcine mammary gland epithelial cells proliferation and lipid metabolism.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!