Aromatase inhibition by 5-substituted pyrimidines and dihydropyrimidines

…, JD Davenport, KS Hirsch, TJ Kress…

Index: Taylor, Harold M.; Jones, C. David; Davenport, James D.; Hirsch, Kenneth S.; Kress, T.J.; Weaver, Dix Journal of Medicinal Chemistry, 1987 , vol. 30, # 8 p. 1359 - 1365

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Citation Number: 24

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 ...