Biological evaluation of 5-substituted pyrimidine derivatives as inhibitors of brassinosteroid biosynthesis
A series of 5-substituted pyrimidine derivatives was synthesized, and their ability to inhibit brassinosteroid biosynthesis was tested. The biological activity of these compounds was evaluated by the cress stem elongation method. Among the synthesized com
Aromatase Inhibition by 5-Substituted Pyrimidines and Dihydropirimidines
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.
Taylor, Harold M.,Jones, C. David,Davenport, James D.,Hirsch, Kenneth S.,Kress, T.J.,Weaver, Dix
p. 1359 - 1365
(2007/10/02)
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