Novel niclosamide-derived Schiff bases as a dual-targeted anticancer agents
Magda M. F. Ismail, Tamer M. Nasr, Moustafa S. Abusaif, Abeer S. Abdelmoniem, Yousry A. Ammar
TL;DR
Researchers developed new niclosamide-based compounds that show strong anticancer effects by targeting two enzymes and inducing cell death in cancer cells.
Contribution
The study introduces niclosamide-derived Schiff bases with dual inhibition of JAK1 and CDK7 enzymes, showing enhanced anticancer activity.
Findings
Compound 11 exhibited strong anticancer activity with IC50 values of 2.85 µM in MCF-7 cells.
Compound 11 induced cell cycle arrest and increased apoptosis in cancer cells more effectively than niclosamide.
Molecular docking confirmed the dual inhibitory effects of compounds 8 and 11 on JAK1 and CDK7 enzymes.
Abstract
Nicosamide (NIC), an approved anthelmintic medication, has demonstrated encouraging antitumor action. To enhance NIC’s pharmacokinetic and pharmacodynamic characteristics and make it a potential anticancer drug, thirteen NIC-Schiff bases were created by condensation reaction of NIC-amine 2 with various monocyclic/bicyclic/tricyclic aromatic aldehydes/acetophenone in absolute ethanol. Several spectroscopic methods, such as elemental analysis, IR, ¹H NMR, and MS, were used to determine the structures of these novel synthesized compounds. MTT assay was used to assess the target compounds’ activity against prostate cancer cell line (PC-3) and two breast cancer cell lines (MCF-7) and (MDA-MB-231). IC50 was determined for the most promising compounds using doxorubicin and NIC as reference standards. Among the compounds examined, the noteworthy compound 11 exhibited IC50 values of 2.85, 4.61,…
Genes, proteins, chemicals, diseases, species, mutations and cell lines named across the full text — each resolved to its canonical identifier and authoritative record.
Click any figure to enlarge with its caption.
Figure 10
Figure 11
Figure 12
Figure 13
Figure 14
Figure 15
Figure 16
Figure 17
Figure 18
Figure 19
Figure 1
Figure 20
Figure 2
Figure 3
Figure 4
Figure 5
Figure 6
Figure 7
Figure 8
Figure 9Peer Reviews
No public reviews on file for this paper yet. If you reviewed it on a platform where reviews are public (OpenReview, ICLR, NeurIPS, ICML), you can paste yours below so the community can read it here.
Videos
No videos yet. Explain this paper in a talk, walkthrough, or lecture? Add one.
Taxonomy
TopicsCytokine Signaling Pathways and Interactions · Synthesis and biological activity · Chemokine receptors and signaling