Document Report Card

ID: ALA1123802

Journal: J Med Chem

Title: Aromatase inhibition by 5-substituted pyrimidines and dihydropyrimidines.

Authors: Taylor HM, Jones CD, Davenport JD, Hirsch KS, Kress TJ, Weaver D.

Abstract: The inhibition of estrogen biosynthesis has been suggested to be an effective treatment of hormone-dependent diseases, particularly breast cancer. Several series of 5-substituted pyrimidine derivatives have been synthesized and tested for their ability to inhibit the enzyme aromatase (estrogen synthetase). Compounds were evaluated in an in vitro assay that measured the inhibition of rat ovarian microsomal aromatase activity. Greatest inhibitory activity was achieved in the cases of diarylpyrimidinemethanols and diarylpyrimidinyl methanes which were substituted in the 4- and 4'-positions with electron-withdrawing substituents, particularly Cl.

CiteXplore: 3612685

DOI: 10.1021/jm00391a016