药物化学

Design, Synthesis and In vitro Anti-tumor Evaluation of Novel Acrylohydrazide Thioglycosides

Abstract

Galal H. Elgemeie, Nahed M. Fathy, Ayman B. Farag, Ossama M. El- Badry, Ghaneia S. Hassan, Kamelia M Amin and Fathi Halaweish

A facile, convenient and high yielding synthesis of novel Acrylohydrazide thioglycosides via one-pot reaction of the potassium thiolate salts of aglycon part - prepared from readily available starting materials - with 2,3,4,6-tetra-O-acetyl- α-D-gluco- and galactopyranosyl bromides . Pharmacological evaluation of compounds 8j, 8b, 8h, 8k, 8f and 5b in vitro against (MCF-7) cell line (Breast carcinoma cell line) showing high- moderate anti-tumor activities with IC50 values ranging from 3.69-14.93 (μM), moreover molecular modeling of these compounds revealed that they have high binding affinity through hydrophobic-hydrophobic interaction and moderate selectivity through the hydrogen bond interaction with the atypical nucleotide binding pocket in the amino terminus of Hsp90.