15001-40-8

Upstream product

• 14846-63-0 4-nitro-3-benzyloxyestra-1,3,5-triene-17-one 
• 7732-18-5 water 

Downstream Products

• 85359-12-2 3-benzyloxy-4-hydroxy-1,3,5⁽¹⁰⁾-estratrien-17-one 
• 229486-21-9 3-benzyloxy-4-dimethylaminoestra-1,3,5⁽¹⁰⁾-trien-17-one 
• 1083177-86-9 C₃₁H₃₂N₂O₃ 
• 1083177-87-0 C₃₁H₃₂N₂O₃ 
• 1083177-85-8 C₃₁H₃₂N₂O₃ 
• 1083177-88-1 C₂₉H₃₀N₂O₄ 
• 85359-13-3 sodium 3-benzyloxy-4-hydroxy-1,3,5⁽¹⁰⁾-estatrien-17-one 4-sulfate 
• 85359-18-8 sodium 4-hydroxy-3-methoxy-1,3,5(10)-estatrien-17-one 4-sulfate 
• 85359-14-4 sodium 3,4-dihydroxy-1,3,5(10)-estatrien-17-one 4-sulfate 

Relevant academic research and scientific papers

Structure-activity relationships of estrogen derivatives as aromatase inhibitors. Effects of heterocyclic substituents

Aromatase, which is responsible for the conversion of androgens to estrogens, is a potential therapeutic target for the selective lowering estrogen level in patients with estrogen-dependent breast cancer. We prepared and tested series of the pyridine- and other heterocyclic ring-containing derivatives of 2- and 4-aminoestrones, estrone, and estradiol, compounds 5, 10, 12 and 15. The isonicotinyl derivatives of 2- and 4-aminoestrone, compounds 5c and 10c, were fairly potent competitive inhibitors of aromatase (KI, 2.1±0.14 and 1.53±0.08 μm for 5c and 10c, respectively) and other compounds did not show, to a significant extent, the aromatase inhibitory activity. This result suggests that the isonicotinyl-substituted derivatives 5c and 10c would be accessible to the active site of aromatase.

Estrone sulfamate inhibitors of estrone sulfatase, and associated pharmaceutical compositions and methods of use

Novel compounds useful as inhibitors of estrone sulfatase are provided. The compounds have the structural formula (I) wherein r1 is an optional double bond, R1 and R2 are selected from the group consisting of hydrogen and lower alky, or together form a cy