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.
Method & Results: The triazole glycosides were a result of 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. 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.
Keywords: Thiazole, tetrazoles, 1, 2, 3-triazoles, glycosides, CDK-2, docking, breast cancer.
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