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3-carboxamido-1,3,5(10)-estratrien-17(R)-spiro-2'(5',5'-dimethyl-6'oxo)tetrahydropyran

Development stage
Unknown
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
01

Overview

This compound is a synthetic steroid derivative belonging to the class of organic compounds known as steroids and steroid derivatives. It is an experimental small molecule that has not been approved for clinical use. The primary known mechanism of action is potent inhibition of aldo-keto reductase family 1 member C3 (AKR1C3), also known as 17β-hydroxysteroid dehydrogenase type 5. AKR1C3 plays a key role in androgen and estrogen metabolism and prostaglandin synthesis. Inhibition of this enzyme may have potential applications in hormone-dependent cancers such as prostate cancer or breast cancer; however, there are no approved indications or advanced clinical trials reported for this compound[1][7][10]. The drug has been studied structurally in complex with its target protein but remains at the experimental stage.

Other names
E04E-04E 04(8R,9S,13S,14S,17R)-5',5',13-trimethyl-6'-oxo-spiro[cyclopenta[a]phenanthrene-17,2'-pyran]-3-carboxamideSpiro[17H-cyclopenta[a]phenanthrene-17,2′-[2H]pyran]-3-carboxamide
02

Targets

AKR1C3 (Aldo-keto reductase family 1 member C3)

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