Journal of medicinal chemistry

Aromatase inhibitors. Synthesis and evaluation of mammary tumor inhibiting activity of 3-alkylated 3-(4-aminophenyl) piperidine-2, 6-diones

RW Hartmann, C Batzl

Index: Hartmann, Rolf W.; Batzl, Christine Journal of Medicinal Chemistry, 1986 , vol. 29, # 8 p. 1362 - 1369

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Citation Number: 126

Abstract

The synthesis and biological evaluation of 3-alkyl-substituted 3-(4-aminophenyl) piperidine- 2, 6-diones asinhibitors of estrogen biosynthesis are described [H (l), methyl (2), ethyl (3), n- propyl (4), isopropyl (5), n-butyl (6), isobutyl (7), sec-butyl (8), n-pentyl (9), isopentyl (lo), 2- methylbutyl (ll), sec-pentyl (12), n-hexyl (13), n-heptyl (14) l. In vitro compounds 4-14 showed a stronger inhibition of human placental aromatase compared to ...