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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
- 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.
- Subjects :
- Pyrazole
Antiproliferative
RIP 1 kinase inhibitor
Pancreatic cancer
Chemistry
QD1-999
Subjects
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