Synthesis and Structure–Activity Relationship Studies of Derivatives of the Dual Aromatase–Sulfatase Inhibitor 4??{[(4??Cyanophenyl)(4H??1, 2, 4??triazol??4??yl) …

LW Woo, PM Wood, C Bubert, MP Thomas…

Index: Woo, L. W. Lawrence; Wood, Paul M.; Bubert, Christian; Thomas, Mark P.; Purohit, Atul; Potter, Barry V. L. ChemMedChem, 2013 , vol. 8, # 5 p. 779 - 799

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Citation Number: 8

Abstract

Abstract 4-{[(4-Cyanophenyl)(4H-1, 2, 4-triazol-4-yl) amino] methyl} phenyl sulfamate and its ortho-halogenated (F, Cl, Br) derivatives are first-generation dual aromatase and sulfatase inhibitors (DASIs). Structure–activity relationship studies were performed on these compounds, and various modifications were made to their structures involving relocation of the halogen atom, introduction of more halogen atoms, replacement of the halogen with ...