Synthesis and biochemical evaluation of inhibitors of estrone sulfatase

James, Karen Elizabeth (2000) Synthesis and biochemical evaluation of inhibitors of estrone sulfatase. (PhD thesis), Kingston University, .


The use of enzyme inhibitors in the treatment of patents with hormone-dependant breast cancer is discussed. Particular emphasis is placed on the inhibition of the enzymes 17[beta]-hydroxysteroid dehydrogenase, aromatase, and estrone sulfatase. Novel inhibitors of estrone sulfatase have been designed, synthesised, and subsequently subjected to biochemical testing to assess their inhibitory activity. From this study a number of highly potent non-steroidal compounds have been identified which appear to be the most potent non-steroidal estrone sulfatase inhibitors known to date. Investigation into the structural activity relationships that exist within the sulfamate-containing inhibitors has been undertaken, and a correlation has been identified between the p[kappa][sub]a of the parent phenol compound and the potency of the sulfamate derivative against estrone sulfatase. Finally, the design, synthesis, and biochemical evaluation of dual inhibitors of estrone sulfatase and aromatase has begun. These studies have helped to identify potential new lead compounds in the treatment of hormone dependent breast cancer.

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