1421036-69-2

Upstream product

• 1421036-68-1 3,3-ethylenedioxy-5α,17β-dihydroxy-17-(1,1,2,2,2-pentafluoroethyl)-11β-[4'-(hydroxymethyl)phenyl]-estr-9-ene 
• 1421036-67-0 3,3-ethylenedioxy-5α,17β-dihydroxy-17-(1,1,2,2,2-pentafluoroethyl)-11β-[4'-(tert-butyldimethylsilyloxymethyl)phenyl]-estr-9-ene 
• 1421036-66-9 3,3-ethylenedioxy-5α,10α-epoxy-17β-hydroxy-17-(1,1,2,2,2-pentafluoroethyl)-estra-9(11)-ene 
• 5571-36-8 ethylene deltenone 

Downstream Products

• 1422447-21-9 17β-hydroxy-17α-(1,1,2,2,2-pentafluoroethyl)-11β-[4'-(2'2'2'-trifluoracetyl)phenyl]-estra-4,9-dien-3-one 
• 1422259-33-3 17β-hydroxy-17α-(1,1,2,2,2-pentafluoroethyl)-11β-{4'-[1'-hydroxy-2'2'2'-trifluoroethyl]phenyl}-estra-4,9-dien-3-one 
• 1421036-70-5 C₃₂H₃₉F₅O₅ 

Relevant academic research and scientific papers

Synthesis and biological evaluation of partially fluorinated antiprogestins and mesoprogestins

A series of antiprogestins have been synthesized by partially fluorinating the steroid molecule in positions relevant for receptor binding. By introducing fluorine at the exo-methylene of the 17 spirofuran ring, we obtained partial agonists (mesoprogestins) with significant applications for antiproliferative and antiovulatory treatment strategies in gynecological therapy such as uterine fibroids, endometriosis and heavy menstrual bleeding. Compared to the standard drug RU486, our synthesized compounds exhibited considerable dissociation between antiprogestational and antiglucocorticoid PR receptors. Furthermore, our studies have shown that pure antiprogestins can be generated by partially fluorinating the 17 propenyl and propynl group or by substituting the 4′ acetyl phenyl group in the 11 position using trifluromethyl group.

PROGESTERONE ANTAGONISTS

Described herein are compounds which either act as pure antiprogestins or as antiprogestins with partial agonistic activity and methods of treating cancer using such compounds.