alexa Design, Synthesis and In vitro Anti-tumor Evaluation of Novel Acrylohydrazide Thioglycosides
ISSN: 2161-0444

Medicinal Chemistry
Open Access

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Research Article

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

Galal H. Elgemeie1*, Nahed M. Fathy2, Ayman B. Farag3, Ossama M. El-Badry3, Ghaneia S. Hassan4, Kamelia M Amin4 and Fathi Halaweish5

1Helwan University, Faculty of Science, Chemistry Department, Ain Helwan, Egypt

2National Research Center, Chemistry Department, Dokki, Egypt

3Ahram Canadian University, Faculty of Pharmacy, Pharmaceutical Chemistry, Giza, Egypt

4Cairo University, Faculty of Pharmacy, Pharmaceutical Chemistry, Cairo, Egypt

5South Dakota University, Faculty of Science, Chemistry Department, USA

*Corresponding Author:
Galal H. Elgemeie
Helwan University, Faculty of Science
Chemistry Department, Ain Helwan, Egypt
2National Research Center, Chemistry Department, Dokki, Egypt
Tel/Fax: 0020225552468
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.

Abstract

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.

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