Chemical and Pharmaceutical Bulletin p. 291 - 296 (1997)
Update date:2022-08-03
Topics:
Matsuno, Toshiyuki
Kato, Masanobu
Tsuchida, Yoshio
Takahashi, Masayuki
Yaguchi, Sin-Ichi
Terada, Sumio
Triamino-substituted 1,3,5-triazine derivatives were synthesized and tested for inhibitory activities against the aromatase of human placental microsomes and the cytochrome P450 side chain cleavage of cholesterol (P450(SCC)) of pig adrenal mitochondria. The compounds having imidazolyl and tertiary amino groups as substituents in the 1,3,5-triazine ring showed significant aromatase-inhibitory activity. Among them, compounds 17, 23, 26, 27 and 28 were more active than the reference compound, CGS 16949A. The inhibitory activities of these compounds against P450(SCC) were much weaker than their aromatase-inhibitory activities. These compounds may be regarded as selective aromatase inhibitors.
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