Design, Synthesis and Anticancer Activity of New Thiazole-Tetrazole or Triazole Hybrid Glycosides Targeting CDK-2 via Structure-Based Virtual Screening.
| Autor: | Kassem AF; Chemistry of Natural and Microbial products Department, National Research Centre, El-Behouth St, Dokki, Cairo, Egypt., Abbas EMH; Chemistry of Natural and Microbial products Department, National Research Centre, El-Behouth St, Dokki, Cairo, Egypt., El-Kady DS; Hormone Department, National Research Centre, El-Behouth St, Dokki, Cairo, Egypt., Awad HM; Tanning Materials and Leather Technology Department, National Research Centre, El-Behouth St, Dokki, Cairo, Egypt., El-Sayed WA; Chemistry Depart- ment, Faculty of Science, Qassim University, Al-Qassim, Kingdom of Saudi Arabia.; Photochemistry Department, National Research Centre, El-Behouth St, Dokki, Cairo, Egypt. |
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| Jazyk: | angličtina |
| Zdroj: | Mini reviews in medicinal chemistry [Mini Rev Med Chem] 2019; Vol. 19 (11), pp. 933-948. |
| DOI: | 10.2174/1389557519666181231121217 |
| Abstrakt: | Background & Objective: The target tetrazole glycosides were synthesized by construction of ring system by cycloaddition reaction of benzothiazole-linked nitrile derivative and sodium azide followed by N-glycosylation process and deprotection. Methods: The triazole glycosides were prepared by applying click approach involving dipolar cycloaddition of benzothiazole possessing alkyne functionality and different glycosyl azides. The products incorporating acyclic analogs of sugar moieties were synthesized through alkylation using acyclic oxygenated halides. Results: The anticancer activity was studied against human breast adenocarcinoma cells (MCF-7) and human normal Retina pigmented epithelium cells (RPE-1). High activities were revealed by three compounds with IC50 values 11.9-16.5 µM compared to doxorubicin (18.6 µM) in addition to other four derivatives with good inhibition activities. Conclusion: Enzyme docking investigation was performed into cyclin-dependent kinase 2 (CDK2); a potential target for cancer medication. Compounds which have possessed highest activities revealed good fitting inside the binding site of the protein molecular surface and showed minimum binding energy. (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.) |
| Databáze: | MEDLINE |
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