Document Type : Original Article
Authors
1
Department of Chemistry, Faculty of Science, University of Cairo, Giza, 12613, Egypt
2
Polymers & Pigments Department, Industrial Chemical Institute, National Research Centre, 33 El-Behouth St. Dokki, Cairo, Egypt.
3
Therapeutic Chemistry Department, Pharmaceutical and Drug Industries Institute, National Research Centre, 33 El-Behouth St. Dokki, Cairo, Egypt.
4
Chemistry 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.
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