Abstract

Fawzia Z. El-Ablack*, Samuel Tanas Melek and Noha Yehia Eid

ABSTRACT

In recent years, heterocyclic compounds are acquiring more importance because of their wide spectrum of biological and pharmacological activities. Also, exhibit exciting medicinal properties including anticancer. The rhodanine (2-thioxothiazolidin-4-one) derivatives are considered as the privileged heterocyclic system in modern medicinal chemistry especially in the discovery of new anticancer agents due to their great affinity to many anticancer biotargets. In the present study, newly designed rhodamine -based derivative 8-imino-9-(4-nitrophenyl)-7-phenyl-5,7,8,9-tetrahydro-2H thiazolo [5',4':5,6] pyrano [2,3-d] pyrimidine-2,6(3H)-dithione (N2) was synthesized to evaluate its anticancer potential against Ehrlich Ascites tumor (EAC) bearing mice. The antitumor effect was assessed by evaluating tumor volume, tumor cell count, survival time and increase in the life span of EAC bearing mice also improvement of hematological status and food intake. The therapeutic impact of three consecutive doses of N2 was used comparing with the traditional drug 5-FU (5-flurouracil) and their mix. A total of 90 female adult Swiss albino mice were randomly divided into nine groups (n=10). Inoculation of 2.5x106 EAC in all treated groups followed by different doss's injection of the (N2) compound to prove its antitumor effect, the ability to improve hematological parameters and food intake compared to positive EAC (Ehrlich ascites carcinoma) group. Normal mice were treated with compound of dose (100 mg/kg) to show its low toxicity effect compared to negative normal group and also treated with DMSO to the same reason. Our results demonstrated that the new compound N2 significantly reduced ascites tumor volume, cell number, and increased the life span of EAC-bearing mice. In addition, the new compound N2 can return the hematological parameters to their normal levels mice also managed to regain their appetite by increasing the dose in dose dependent manner. The highest dose of the compound and the 5-FU gave similar results and their mix group gave us the best result ever. From our findings, it is noted that the N2 derivative may be possible candidate for anticancer therapy with the ability to inhibit tumor cell proliferation.