Química medicinal

Design, Synthesis and Cytotoxic Evaluation of Novel Heterocyclic Thioglycosides

Abstract

Elgemeie GH, Farag AB, Amin KM, El-Badry OM and Hassan GS

A novel series of 2-thioxoimidazolidin-4-one and Benzothiazole thioglycosides were synthesized via one-pot reaction of the 2-thioxoimidazolidin-4-one and Benzothiazole thiolate salts, respectively with 2,3,4,6-tetra-O-acetyl- α-D-gluco- and galactopyranosyl bromides. The cytotoxic activity of compound 7, 8a, 8b, 10a, 10b, 15a and 15b were evaluated against MCF-7 cell lines (Breast carcinoma cell lines) showing high to moderate anti-tumor activities moreover molecular modeling of these compounds revealed that they have high binding affinity through hydrophobichydrophobic interaction and moderate selectivity through the hydrogen bond interaction with the atypical nucleotide binding pocket in the amino terminus of HSP90.