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Bis-pyrazole as receptor interacting protein 1 kinase inhibitor: Synthesis, preliminary biological evaluation against pancreatic cancer cell line and its docking studies

Authors :
Sandeep Singh
Rajeev Kumar Sharma
R. Ramajayam
Source :
Results in Chemistry, Vol 7, Iss , Pp 101447- (2024)
Publication Year :
2024
Publisher :
Elsevier, 2024.

Abstract

The pyrazole heterocycle displayed versatile pharmacological activity ranging from anti-inflammatory to antiviral. Herein, we report the synthesis of bis-pyrazole as receptor- interacting protein 1 kinase inhibitor and evaluated for antiproliferative activity against pancreatic cancer line, PANC-1. Among twelve compounds, three candidates displayed the cytotoxicity IC50 value in single digit micromolar concentration. From the preliminary evaluation, the compound 31 emerged as a potential inhibitor with an IC50 = 4.1 µM. The lead compound showed similar inhibitor IC50 value in comparison to the positive control, doxorubicin. The docking studies confirm that these analogs may require further investigation to improve the potency.

Details

Language :
English
ISSN :
22117156
Volume :
7
Issue :
101447-
Database :
Directory of Open Access Journals
Journal :
Results in Chemistry
Publication Type :
Academic Journal
Accession number :
edsdoj.970ec2f94a96409fa18e983c8367e72c
Document Type :
article
Full Text :
https://doi.org/10.1016/j.rechem.2024.101447