Antitumor activities of new iso(thio)cyanates and their nitrogen and sulphur heterocyclic phosphorus derivatives

Abstract

The cytotoxic activity of Iso(thio)cyanate derivatives and some new organophosphorus compounds were determined, using MTT assay against human hepatocellular carcinoma (HepG2) and adenocarcinoma breast (MCF-7) in comparison with the reference drug 5-flurouracil. All the selected products have been tested and showed concentration dependent increase in the growth inhibition percentage against HepG2 and MCF-7. Where, the thietane derivatives revealed anticancer activity with IC 50 (20, 8.9 μg/ml) against HepG2 and (20, 10.3 μg/ml) against MCF-7; while, thiazinane compounds showed IC 50 (12.7, 32.5 μg/ml) against HepG2 and (20 and 20 μg/ml) against MCF-7. The newly synthesized azetidines showed anticancer activity with IC 50 (13.5 and 32.5 μg/ml) against HepG2 and IC 50 (10 and 25.9 μg/ml) against MCF-7 cancer. Moreover, azetidinedione compound exhibited more potent activity than the azetidinone with both types of cancer cell lines. In addition, the cytotoxic activity of the iso(thio)cyanates, and malonamic acid methyl ester compound were also investigated. 4-Methoxyphenyl isothiocyanate and methylisothiocyanate, with IC 50 (25.9, 12.3 and 40, 20 μg/ml), respectively, against HepG2 and MCF-7 cancer cells. 1, 2-Dichloro-4-isocyanato-benzene was similar in potency to the known anticancer drug 5-flurouracil with IC 50 (5.3 μg/ml) versus 5 μg/ml for 5-flurouracil against MCF-7. While, malonamic acid methyl ester compound had no effect on both types of cancer cell lines.