Highly Potent First Examples of Dual Aromatase− Steroid Sulfatase Inhibitors based on a Biphenyl Template†

…, T Jackson, A Putey, G Cozier, P Leonard…

文献索引：Lawrence Woo; Jackson, Toby; Putey, Aurelien; Cozier, Gyles; Leonard, Philip; Ravi Acharya; Chander, Surinder K.; Purohit, Atul; Reed, Michael J.; Potter, Barry V. L. Journal of Medicinal Chemistry, 2010 , vol. 53, # 5 p. 2155 - 2170

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被引用次数: 52

摘要

Single agents against multiple drug targets are of increasing interest. Hormone-dependent breast cancer (HDBC) may be more effectively treated by dual inhibition of aromatase and steroid sulfatase (STS). The aromatase inhibitory pharmacophore was thus introduced into a known biphenyl STS inhibitor to give a series of novel dual aromatase− sulfatase inhibitors (DASIs). Several compounds are good aromatase or STS inhibitors and DASI 20 (IC50: ...