PTSA-induced synthesis, in silico and nano study of novel ethylquinolin-thiazolo-triazole in cervical cancer
Aim: p-Toluenesulfonic acid-(PTSA) and grinding-induced novel synthesis of ethylquinolin-thiazolo-triazole derivatives was performed using green chemistry. Materials & methods: Development of a nanoconjugate drug-delivery system of ethylquinolin-thiazolo-triazole was carried out with D-α-tocopheryl polyethylene glycol succinate (TPGS) and the formulation was further characterized by transmission electron microscopy, atomic force microscopy, dynamic light scattering and in vitro drug release assay. The effect of 3a nanoparticles was assessed against a cervical cancer cell line (HeLa) through the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, and the effect on apoptosis was determined. Results & discussion: The 3a nanoparticles triggered the apoptotic mode of cell death after increasing the intracellular reactive oxygen level by enhancing cellular uptake of micelles. Furthermore, in silico studies revealed higher absorption, distribution, metabolism, elimination and toxicity properties and bioavailability of the enzyme tyrosine protein kinase. Conclusion: The 3a nanoparticles enhanced the therapeutic potential and have higher potential for targeted drug delivery against cervical cancer.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2024 |
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| Erschienen: |
2024 |
| Enthalten in: |
Zur Gesamtaufnahme - year:2024 |
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| Enthalten in: |
Future medicinal chemistry - (2024) vom: 10. Apr. |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Sonker, Priyanka [VerfasserIn] |
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| Links: |
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| Themen: |
ADMET |
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| Anmerkungen: |
Date Revised 10.04.2024 published: Print-Electronic Citation Status Publisher |
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| doi: |
10.4155/fmc-2023-0344 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM370862384 |
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| LEADER | 01000naa a22002652 4500 | ||
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| 100 | 1 | |a Sonker, Priyanka |e verfasserin |4 aut | |
| 245 | 1 | 0 | |a PTSA-induced synthesis, in silico and nano study of novel ethylquinolin-thiazolo-triazole in cervical cancer |
| 264 | 1 | |c 2024 | |
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| 500 | |a Date Revised 10.04.2024 | ||
| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status Publisher | ||
| 520 | |a Aim: p-Toluenesulfonic acid-(PTSA) and grinding-induced novel synthesis of ethylquinolin-thiazolo-triazole derivatives was performed using green chemistry. Materials & methods: Development of a nanoconjugate drug-delivery system of ethylquinolin-thiazolo-triazole was carried out with D-α-tocopheryl polyethylene glycol succinate (TPGS) and the formulation was further characterized by transmission electron microscopy, atomic force microscopy, dynamic light scattering and in vitro drug release assay. The effect of 3a nanoparticles was assessed against a cervical cancer cell line (HeLa) through the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, and the effect on apoptosis was determined. Results & discussion: The 3a nanoparticles triggered the apoptotic mode of cell death after increasing the intracellular reactive oxygen level by enhancing cellular uptake of micelles. Furthermore, in silico studies revealed higher absorption, distribution, metabolism, elimination and toxicity properties and bioavailability of the enzyme tyrosine protein kinase. Conclusion: The 3a nanoparticles enhanced the therapeutic potential and have higher potential for targeted drug delivery against cervical cancer | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a ADMET | |
| 650 | 4 | |a docking | |
| 650 | 4 | |a drug-likeness | |
| 650 | 4 | |a in vitro | |
| 650 | 4 | |a nanoformulation | |
| 650 | 4 | |a synthesis | |
| 700 | 1 | |a Tamang, Rupen |e verfasserin |4 aut | |
| 700 | 1 | |a Mehata, Abhishesh K |e verfasserin |4 aut | |
| 700 | 1 | |a Nidhar, Manisha |e verfasserin |4 aut | |
| 700 | 1 | |a Sharma, Vishal P |e verfasserin |4 aut | |
| 700 | 1 | |a Kumar, Vipin |e verfasserin |4 aut | |
| 700 | 1 | |a Muthu, Madaswamy S |e verfasserin |4 aut | |
| 700 | 1 | |a Koch, Biplob |e verfasserin |4 aut | |
| 700 | 1 | |a Tewari, Ashish K |e verfasserin |4 aut | |
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