Mohammed I. El-Gamal, Mohammad H. Semreen, Ayat E. Abbas, Iman G. Moussa, Israa A. Younis and Youmna Y. Zaghloul
College of Pharmacy, Institute of Medical Research, University of Sharjah, Sharjah 27272, UAE; Sharjah Institute of Medical Research, University of Sharjah, Sharjah 27272, UAE; Department of Medicinal Chemistry, Faculty of Pharmacy, University of Mansoura, Mansoura 35516, Egypt
A new series of arylamide derivatives possessing terminal sulfonate or sulfamate moieties were designed and synthesized. They were tested for inhibitory effect against steroid sulfatase (STS) enzyme for treatment of estrogen- and androgen-dependent cancers. The free sulfamate derivative 1i showed the most promising inhibitory effects in cell-free STS enzyme and in JEG-3 placental carcinoma cells rich in STS. The target compounds were also tested for in vitro antiproliferative activity against a panel of 60 cancer cell lines of nine different cancer types at the National Cancer Institute (NCI, Bethesda, Maryland, USA). The aromatic sulfonate derivatives exerted the most promising results. Three of them were selective against HT 29 colon cancer cell line with high potency and superior selectivity against it than normal fibroblasts. One compound showed broad-spectrum activity against most of the tested cancer types. And another compound was selective against CNS cancer subpanel.