This is a preprint, a preliminary version of a manuscript that has not completed peer review at a journal. Research Square does not conduct peer review prior to posting preprints. The posting of a preprint on this server should not be interpreted as an endorsement of its validity or suitability for dissemination as established information or for guiding clinical practice.
Research Article
Ganesh D. Barkade
Padmashri Doctor Vithalrao Vikhe Patil Foundation's College of Pharmacy
Corresponding Author
ORCiD: https://orcid.org/0000-0003-3836-3125
License:
This work is licensed under a CC BY 4.0 License. Read Full License
Background: Cancer is a leading cause of death worldwide. Inhibiting mitosis is the most effective clinical technique for cancer treatment. The most critical field of medicinal chemistry and drug development research is the discovery of innovative anticancer drugs. Thiazolidine is a multifunctional nucleus with anticancer, anti-inflammatory, antioxidant, antibacterial, antifungal, antidiabetic, antihyperlipidemic, and antiarthritic properties.
Methods: In this investigation, copper-nickel oxide nanoparticles synthesized by electrochemical synthesis yielded a significant yield. The capping was done with cetyltrimethyl ammonium bromide (CTAB), and the characterization was done with UV, FTIR, XRD, SEM-EDS, and TEM SAED. The biologically significant 2-(2-substituted-4-oxo-thiazolidine-3-yl)-1, 9-dihydro-purin-6-ones (GB-1 to GB-12) have been synthesized using copper-nickel oxide nanoparticles as a catalyst and by applying a microwave-assisted tool. It was characterized by melting point, IR, 1H NMR, 13C NMR and LC-HRMS/MS spectroscopy. Using Sulforhodamine B (SRB) test, all newly synthesized compounds were evaluated in vitro for anti-cancer, anti-inflammatory, antioxidant, and angiogenesis activities.
Results: The compounds GB-6 (GI50: 30 μM), GB-8 (GI50: 10 μM) and GB-10 (GI50: 30 μM) exhibited significant cell growth inhibitory activity. The compounds GB-6, GB-8, GB-10 exhibited significant in vitro anti-inflammatory activity in the range of IC50:179.65-194.59 μg/ml as compared with aceclofenac (IC50:191.19μg/ml) and the antioxidant activity by DPPH radical scavenging assay the compounds GB-6 (IC50:11.96 µg/ml), GB-8 (IC50:10.67 µg/ml) and GB-10 (IC50: 9.08 µg/ml) exhibited excellent radical scavenging activities compared to ascorbic acid (IC50:13.04 µg/ml) and by the KMnO4 radical scavenging assay the compounds GB-2 (IC50:15.33 µg/ml), GB-4 (IC50:23.60 µg/ml), GB-8 (IC50:24.93 µg/ml), GB-10 (IC50:24.96 µg/ml) exhibited good radical scavenging activities compared to ascorbic acid (IC50: 26.55 µg/ml). The compounds GB-4, GB-8 and GB-10 at 10 nM test drug concentration and the GB-6 compounds at 100 nM test drug concentration show the maximum capillary growth inhibitory activity compared with thalidomide as a standard drug.
Conclusion: Further development of anticancer drugs may be enabled by the discovery of related compounds to the anticancer agent, such as compound (GB-6), compound (GB-8), and compound (GB-10) as polo-like kinase 1 inhibitors.
Keywords
Nanocatalytic synthesis, Copper nickel oxide nanoparticles, Thiazolidine-4-ones, Anticancer activity, Angiogenesis activity, Antioxidant activity
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This is a preprint, a preliminary version of a manuscript that has not completed peer review at a journal. Research Square does not conduct peer review prior to posting preprints. The posting of a preprint on this server should not be interpreted as an endorsement of its validity or suitability for dissemination as established information or for guiding clinical practice.
Research Article
Ganesh D. Barkade
Padmashri Doctor Vithalrao Vikhe Patil Foundation's College of Pharmacy
Corresponding Author
ORCiD: https://orcid.org/0000-0003-3836-3125
Badges
Prescreen
This manuscript passed our Prescreen assessment
Complete author information
Appropriate declaration statements
Potential risks to human health
Prescreen
History
CURRENT STATUS: Posted
Version 1
Posted 09 Sep, 2021
No community comments so far
Metrics
Comments: 0
PDF Downloads: ...
HTML Views: ...
Subject Areas
Medicinal Chemistry
License:
This work is licensed under a CC BY 4.0 License. Read Full License
Background: Cancer is a leading cause of death worldwide. Inhibiting mitosis is the most effective clinical technique for cancer treatment. The most critical field of medicinal chemistry and drug development research is the discovery of innovative anticancer drugs. Thiazolidine is a multifunctional nucleus with anticancer, anti-inflammatory, antioxidant, antibacterial, antifungal, antidiabetic, antihyperlipidemic, and antiarthritic properties.
Methods: In this investigation, copper-nickel oxide nanoparticles synthesized by electrochemical synthesis yielded a significant yield. The capping was done with cetyltrimethyl ammonium bromide (CTAB), and the characterization was done with UV, FTIR, XRD, SEM-EDS, and TEM SAED. The biologically significant 2-(2-substituted-4-oxo-thiazolidine-3-yl)-1, 9-dihydro-purin-6-ones (GB-1 to GB-12) have been synthesized using copper-nickel oxide nanoparticles as a catalyst and by applying a microwave-assisted tool. It was characterized by melting point, IR, 1H NMR, 13C NMR and LC-HRMS/MS spectroscopy. Using Sulforhodamine B (SRB) test, all newly synthesized compounds were evaluated in vitro for anti-cancer, anti-inflammatory, antioxidant, and angiogenesis activities.
Results: The compounds GB-6 (GI50: 30 μM), GB-8 (GI50: 10 μM) and GB-10 (GI50: 30 μM) exhibited significant cell growth inhibitory activity. The compounds GB-6, GB-8, GB-10 exhibited significant in vitro anti-inflammatory activity in the range of IC50:179.65-194.59 μg/ml as compared with aceclofenac (IC50:191.19μg/ml) and the antioxidant activity by DPPH radical scavenging assay the compounds GB-6 (IC50:11.96 µg/ml), GB-8 (IC50:10.67 µg/ml) and GB-10 (IC50: 9.08 µg/ml) exhibited excellent radical scavenging activities compared to ascorbic acid (IC50:13.04 µg/ml) and by the KMnO4 radical scavenging assay the compounds GB-2 (IC50:15.33 µg/ml), GB-4 (IC50:23.60 µg/ml), GB-8 (IC50:24.93 µg/ml), GB-10 (IC50:24.96 µg/ml) exhibited good radical scavenging activities compared to ascorbic acid (IC50: 26.55 µg/ml). The compounds GB-4, GB-8 and GB-10 at 10 nM test drug concentration and the GB-6 compounds at 100 nM test drug concentration show the maximum capillary growth inhibitory activity compared with thalidomide as a standard drug.
Conclusion: Further development of anticancer drugs may be enabled by the discovery of related compounds to the anticancer agent, such as compound (GB-6), compound (GB-8), and compound (GB-10) as polo-like kinase 1 inhibitors.
Figure 1
Figure 2
Figure 3
Figure 4
Figure 5
Figure 6
Figure 7
Figure 8
Figure 9
Figure 10
Figure 11
Figure 12
Figure 13
Figure 14
Figure 15
Figure 16
This is a list of supplementary files associated with this preprint. Click to download.
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