e.g. Filippa Pettersson or Cancer Res. 75(6) , 1102-12, (2015) or 10.1002/anie.201600521

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

Full Text: HTML

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 ...

Benzyl cyanide Structure

~%

2-ethyl-2-phenylglutaronitrile Structure

2-ethyl-2-pheny...

Butyl iodide Structure

Benzyl cyanide Structure

~64%

2-phenylhexanenitrile Structure

2-phenylhexanen...

2-Iodopropane Structure

Benzyl cyanide Structure

~86%

2-Isopropyl-2-phenylacetonitrile Structure

2-Isopropyl-2-p...

2-phenylbutyronitrile Structure

2-phenylbutyron...

Acrylonitrile Structure

~51%

2-ethyl-2-phenylglutaronitrile Structure

2-ethyl-2-pheny...

1-Iodo-2-methylpropane Structure

1-Iodo-2-methyl...

Benzyl cyanide Structure

~72%

Benzeneacetonitrile, a-(2-methylpropyl)- Structure

Benzeneacetonit...

3-(4-nitrophenyl)piperidine-2,6-dione Structure

3-(4-nitropheny...

~%

3-(4-aminophenyl)piperidine-2,6-dione Structure

3-(4-aminopheny...

3-Phenylpiperidine-2,6-dione Structure

3-Phenylpiperid...

~%

3-(4-aminophenyl)piperidine-2,6-dione Structure

3-(4-aminopheny...

2-Phenylpentanedinitrile Structure

2-Phenylpentane...

~%

3-(4-aminophenyl)piperidine-2,6-dione Structure

3-(4-aminopheny...

Benzyl cyanide Structure

~%

3-(4-aminophenyl)piperidine-2,6-dione Structure

3-(4-aminopheny...

2-phenyl-2-propylpentanedinitrile Structure

2-phenyl-2-prop...

~56%

3-phenyl-3-propylpiperidine-2,6-dione Structure

3-phenyl-3-prop...

Benzyl cyanide Structure

~%

3-phenyl-3-propylpiperidine-2,6-dione Structure

3-phenyl-3-prop...

2-ethyl-2-phenylglutaronitrile Structure

2-ethyl-2-pheny...

~58%

glutethimide Structure

glutethimide Structure

~9%

3-ethyl-3-(4-nitrophenyl)piperidine-2,6-dione Structure

3-ethyl-3-(4-ni...

2-phenylbutyronitrile Structure

2-phenylbutyron...

~%

3-ethyl-3-(4-nitrophenyl)piperidine-2,6-dione Structure

3-ethyl-3-(4-ni...

Benzyl cyanide Structure

~%

3-ethyl-3-(4-nitrophenyl)piperidine-2,6-dione Structure

3-ethyl-3-(4-ni...

2-ethyl-2-phenylglutaronitrile Structure

2-ethyl-2-pheny...

~%

3-ethyl-3-(4-nitrophenyl)piperidine-2,6-dione Structure

3-ethyl-3-(4-ni...