Exploration of Ring Rearrangement Metathesis Reaction: A General and Flexible Approach for the Rapid Construction [5,<i>n</i>]‑Fused Bicyclic Systems en Route to Linear Triquinanes

Structurally diverse [5,<i>n</i>] bicyclic systems with <i>cis</i> ring junction stereochemistry were accessed readily through RRM (ring rearrangement metathesis) reaction of properly functionalized [2.2.1]­norbornene skeletons. Several bicyclic enones, ketones, alcohols, and ethers acted as the substrates and yielded the respective linearly fused [5,<i>n</i>] bicyclic systems stereoselectively after the RRM reaction. Such [5,5]­bicyclic enone scaffolds were then synthetically manipulated to core structural analogue of naturally occurring liner triquinane hirsutene having <i>cis</i>-<i>syn</i>-<i>cis</i> stereochemistry

Exploration of Ring Rearrangement Metathesis Reaction: A General and Flexible Approach for the Rapid Construction [5,<i>n</i>]‑Fused Bicyclic Systems en Route to Linear Triquinanes

Structurally diverse [5,<i>n</i>] bicyclic systems with <i>cis</i> ring junction stereochemistry were accessed readily through RRM (ring rearrangement metathesis) reaction of properly functionalized [2.2.1]­norbornene skeletons. Several bicyclic enones, ketones, alcohols, and ethers acted as the substrates and yielded the respective linearly fused [5,<i>n</i>] bicyclic systems stereoselectively after the RRM reaction. Such [5,5]­bicyclic enone scaffolds were then synthetically manipulated to core structural analogue of naturally occurring liner triquinane hirsutene having <i>cis</i>-<i>syn</i>-<i>cis</i> stereochemistry

Piperidine-2,6-dione derivatives as cereblon-binding agents and their preparation

http://deepblue.lib.umich.edu/bitstream/2027.42/191180/2/WO 2023-183607 Al.pdfDescription of WO 2023-183607 Al.pdf : Published versio

Discovery of ERD3111 as a Potent and Orally Efficacious Estrogen Receptor PROTAC Degrader with Strong Antitumor Activity

http://deepblue.lib.umich.edu/bitstream/2027.42/191183/2/Poster_ERD-3111 paper.pd

Targeting the Estrogen Receptor (ER) for the Treatment of Breast Cancer: Recent Advances and Challenges

Estrogen receptor alpha (ERα) is a well-established therapeutic target for the treatment of ER-positive (ER+) breast cancers. Despite the tremendous successes achieved by tamoxifen, a selective estrogen receptor modulator, and aromatase inhibitors (AIs), resistance to these therapies is a major clinical problem. Therefore, induced protein degradation and covalent inhibition have been pursued as new therapeutic approaches to target ERα. This review summarizes recent progress in the discovery and development of oral selective ER degraders (SERDs), CERANs (complete estrogen receptor antagonists), SERCAs (selective estrogen receptor covalent antagonists), and PROTAC (proteolysis targeting chimera) ER degraders. We focus on those compounds which have been advanced into clinical developmenthttp://deepblue.lib.umich.edu/bitstream/2027.42/177130/2/acs.jmedchem.3c00136.pdfAccepted versionDescription of acs.jmedchem.3c00136.pdf : Published versio

Chroman derivatives as estrogen receptor degraders and their preparation

http://deepblue.lib.umich.edu/bitstream/2027.42/192162/2/WO2024015409A1_Original_document_20240124172149.pd

Indazole derivatives as estrogen receptor degraders

http://deepblue.lib.umich.edu/bitstream/2027.42/192160/2/WO2024015408A1_Original_document_20240124172255.pd

Indole derivatives as estrogen receptor degraders and their preparation

http://deepblue.lib.umich.edu/bitstream/2027.42/192159/2/WO2024015406A1_Original_document_20240124172356.pd

Cereblon ligands and uses thereof

http://deepblue.lib.umich.edu/bitstream/2027.42/192158/2/WO2024015340A1_Original_document_20240124172503.pdfhttp://deepblue.lib.umich.edu/bitstream/2027.42/192158/3/WO2024015340A1_Original_document_20240124172503.pd

Tetrahydronaphthalene derivatives as estrogen receptor degraders

http://deepblue.lib.umich.edu/bitstream/2027.42/192161/2/WO2024015412A1_Original_document_20240124171942.pd