Der Pharma Chemica
Journal for Medicinal Chemistry, Pharmaceutical Chemistry, Pharmaceutical Sciences and Computational Chemistry

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Abstract

Design, Synthesis, Cytotoxicity, Physicochemical and In Vivo Studies of New Thalidomide Dithiocarbamate Analogs as Anticancer

Author(s): Magdy AH Zahran*, Ayman R Awad, Ahmed BM Mehany and Roba Talaat

Novel thalidomide dithiocarbamate analogs were synthesized in good yield. A two-step synthesis was utilized to obtain the new thalidomide dithiocarbamate analogs by reaction of thalidomide with 1,2 dichloroethane or 1,3 dichloropropane producing chloroethyl thalidomide 2 or chloropropyl thalidomide 3 compounds respectively, which reacts with Sodium diethyl dithiocarbamate to afford thalidomide dithiocarbamate 4 or 5.

 

The chemical structures of all synthesized compounds were elucidated on the basis of their spectral IR, 1H NMR, 13C NMR, Mass spectroscopy and elemental analysis. The anticancer nature of thalidomide and thalidomide analogs 2-5 was evaluated by screening the in vitro activity on three human cancer cell lines; human lung cancer cells (A-549), human liver cancer cells (HEGP-2) and human breast cancer cells (MCF-7). Also the in vivo activity of analogs towards lung cancer was evaluated. Moreover, the physicochemical properties of Thalidomide and their dithiocarbamate analogs were also determined using Mastersizer X.

 

Therefore, thalidomide dithiocarbamate analogs 4 and 5 possess a potential anticancer activity to be formulated as inhaler for lung cancer treatment.

 

Synthesis of new thalidomide dithiocarbamate analogs with anticancer activity and improved physicochemical properties. Thalidomide and thalidomide analogs 2-5 were evaluated for anticancer potency against A-549, MCF-7, HEGP-2 and were also evaluated in vivo towards lung cancer. Moreover, their physicochemical properties were presented as their particle size. These new thalidomide dithiocarbamate analogs 4 and 5 have cytotoxicity against lung cancer cells with IC50 10.4 ± 0.2 µg/ml for compound 4 and IC50 12.4 ± 0.2 µg/ml for compound 5. Also they have small particle size, their improved physicochemical properties together with their anticancer activity, enhance their potential to be formulated as inhaler for lung cancer treatment.


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