Zhang, Zhuming; Connolly, Peter J.; Trabalon Escolar, Luis; Rocaboy, Christian; Pande, Vineet; Meerpoel, Lieven; Lim, Heng-Keang; Branch, Jonathan R.; Ondrus, Janine; Hickson, Ian; Bush, Tammy L.; Bischoff, James R.; Bignan, Gilles published their research in ACS Medicinal Chemistry Letters in 2021. The article was titled 《Spirocyclic Thiohydantoin Antagonists of F877L and Wild-Type Androgen Receptor for Castration-Resistant Prostate Cancer》.Formula: C10H19NO3 The article contains the following contents:
Androgen receptor (AR) transcriptional reactivation plays a key role in the development and progression of lethal castration-resistant prostate cancer (CRPC). Recurrent alterations in the AR enable persistent AR pathway signaling and drive resistance to the treatment of second-generation antiandrogens. AR F877L, a point mutation in the ligand binding domain of the AR, was identified in patients who acquired resistance to enzalutamide or apalutamide. In parallel to our previous structure-activity relationship (SAR) studies of compound 4 (JNJ-pan-AR) and clin. stage compound 5 (JNJ-63576253), we discovered addnl. AR antagonists that provide opportunities for future development. Here we report a highly potent series of spirocyclic thiohydantoins as AR antagonists for the treatment of the F877L mutant and wild-type CRPC. A chirally pure enantiomer,(R)-29 (I) is a full antagonist against AR F877L. In the part of experimental materials, we found many familiar compounds, such as tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Formula: C10H19NO3)
tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas:109384-19-2) is a 4-hydroxypyridine with a boc protecting group used in the preparation of neurologically active agents and other pharmaceutical compounds.Formula: C10H19NO3
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem