Design, Synthesis and In vitro Anti-tumor Evaluation of Novel Acrylohydrazide Thioglycosides
- *Corresponding Author:
- Galal H. Elgemeie
Helwan University, Faculty of Science
Chemistry Department, Ain Helwan, Egypt
2National Research Center, Chemistry Department, Dokki, Egypt
E-mail: [email protected]
Received date: March 12, 2014; Accepted date: April 29, 2014; Published date: May 01, 2014
Citation: Elgemeie GH, Fathy NM, Farag AB, El-Badry OM, Hassan GS, et al. (2014) Design, Synthesis and In vitro Anti-tumor Evaluation of Novel Acrylohydrazide Thioglycosides. Med chem 4:400-406. doi: 10.4172/2161-0444.1000171
Copyright: © 2014 Elgemeie GH, et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.
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.