Tricyclic Indazoles-A Novel Class of Selective Estrogen Receptor Degrader Antagonists was written by Scott, James S.;Bailey, Andrew;Buttar, David;Carbajo, Rodrigo J.;Curwen, Jon;Davey, Paul R. J.;Davies, Robert D. M.;Degorce, Sebastien L.;Donald, Craig;Gangl, Eric;Greenwood, Ryan;Groombridge, Sam D.;Johnson, Tony;Lamont, Scott;Lawson, Mandy;Lister, Andrew;Morrow, Christopher J.;Moss, Thomas A.;Pink, Jennifer H.;Polanski, Radoslaw. And the article was included in Journal of Medicinal Chemistry in 2019.COA of Formula: C8H15NO5S This article mentions the following:
Tricyclic tetrahydropyridoindazoles such as I were prepared as estrogen receptor degrader antagonists for potential use in the treatment of ERα-dependent breast cancer; the indazole moiety was prepared as a replacement for a phenol moiety in a tetrahydroisoquinolinol which generated reactive metabolites in a glutathione trapping assay. The structure of a nonracemic tetrahydropyridoindazole bound to an ERα ligand binding domain fragment was determined by X-ray crystallog. I demonstrated the desired estrogen receptor α degrader-antagonist profile and demonstrated activity in a xenograft model of breast cancer. In the experiment, the researchers used many compounds, for example, (R)-3-Boc-4-methyl-1,2,3-oxathiazolidine 2,2-Dioxide (cas: 454248-53-4COA of Formula: C8H15NO5S).
(R)-3-Boc-4-methyl-1,2,3-oxathiazolidine 2,2-Dioxide (cas: 454248-53-4) belongs to thiazolidine derivatives. Thiazolidine is a heterocyclic compound with five-membered saturated ring with a thioether group and an amine group in 1 and 3 positions of the ring. Thiazolidines have been applied as prodrug derivatives for various steroids containing a 3-carbonyl group to improve their topical anti-inflammatory activity. COA of Formula: C8H15NO5S
Referemce:
Thiazolidine – Wikipedia,
Thiazolidine – ScienceDirect.com