In Sight into Innovative Cancer Therapeutic Approach Based on Nanotechnology: Chitosan (CS) / Polyvinyl alcohol (PVA) Films loaded with Synthesized Bisthiazole Derivative for Cancer Treatment | ||||
| Egyptian Journal of Chemistry | ||||
| Volume 66, Issue 13, December 2023, Page 1997-2011 PDF (1.2 MB) | ||||
| Document Type: Original Article | ||||
| DOI: 10.21608/ejchem.2023.243862.8757 | ||||
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| Authors | ||||
Manar Ayman1; Sobhi M. Gomha1; Magda A. Abdallah1; doaa E. ElNashar2; AbdelMohsen M. Soliman3; Huda R. M. Rashdan  4
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| 1Department of Chemistry, Faculty of Science, University of Cairo, Giza, 12613, Egypt | ||||
| 2Polymers & Pigments Department, Industrial Chemical Institute, National Research Centre, 33 El-Behouth St. Dokki, Cairo, Egypt. | ||||
| 3Therapeutic Chemistry Department, Pharmaceutical and Drug Industries Institute, National Research Centre, 33 El-Behouth St. Dokki, Cairo, Egypt. | ||||
| 4Chemistry of Natural and Microbial Products Department, Pharmaceutical and Drug Industries Research Institute, National Research Centre, 33 El Buhouth St, Dokki, Giza 12622, Egypt. | ||||
| Abstract | ||||
| Acetyl thiazole thiosemicarbazone 3 was used as key intermediate for preparation of novel series of thiazolylhydrazono thiazole derivatives via reaction of 3 with two types of hydrazonoyl halides. Also, compound 3 reacts with alphahaloketones and alphhaloester in ethanol or in acetic acid containing anhydrous sodium acetate under reflux to give another new thiazole based compounds. Addionally, the key intermediate 3 was utilized for synthesis of functionalized thiazolehydrazonothiazolones via its reaction with a variety of compounds containing activated double or triple bonds vis maleic anhydride and dimethyl acetylene dicarboxylate. All spectroscopic techniques (IR,1 HNMR and C13NMR, Mass) and elemental analysis were used for confirmation of all the new synthesized compounds. Moreover, the synthetic mechanism of most of the newly developed compounds was discussed. The as-prepared compounds were screened for their in vitro antiproliferative potential towards different human cell lines, including: colon (LoVo), and liver (HEPG2) and breast (MCF7) cancer cell lines. Results revealed that compounds 1, 6a, 6b and 6e were the most potent against tested cancer cell lines. Moreover, compound 6e was chosen for a further drug delivery study through using chitosan and PVA polymer film as drug carrier. This drug delivery system was used for in vitro anticancer evaluation and genotoxic investigation compared to Doxorubicin. colon (LoVo) cells were treated with various concentrations from the selected compound 6e loaded in CS/PVA drug delivery in comparison to doxorubicin to evaluate its anticancer activity and then analyzed via comet assay to study genotoxicity. | ||||
| Keywords | ||||
| Thiazoles; bisthiazoles, thiosemicarbazones, hydrazonoyl halides; drug delivery; anticancer activity | ||||
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