300627-43-4Relevant articles and documents
Chemical degradation of androgen receptor (Ar) using bicalutamide analog–thalidomide protacs
Kim, Ga Yeong,Song, Chae Won,Yang, Yo-Sep,Lee, Na-Rae,Yoo, Hyung-Seok,Son, Seung Hwan,Lee, Soo Jin,Park, Jong Seon,Lee, Jong Kil,Inn, Kyung-Soo,Kim, Nam-Jung
, (2021/05/26)
A series of PROTACs (PROteolysis-TArgeting Chimeras) consisting of bicalutamide analogs and thalidomides were designed, synthesized, and biologically evaluated as novel androgen receptor (AR) degraders. In particular, we found that PROTAC compound 13b could successfully demonstrate a targeted degradation of AR in AR-positive cancer cells and might be a useful chemical probe for the investigation of AR-dependent cancer cells, as well as a potential therapeutic candidate for prostate cancers.
Identification and optimization of a novel series of [2.2.1]-oxabicyclo imide-based androgen receptor antagonists
Salvati, Mark E.,Balog, Aaron,Shan, Weifang,Rampulla, Richard,Giese, Soren,Mitt, Tom,Furch, Joseph A.,Vite, Gregory D.,Attar, Ricardo M.,Jure-Kunkel, Maria,Geng, Jieping,Rizzo, Cheryl A.,Gottardis, Marco M.,Krystek, Stanley R.,Gougoutas, Jack,Galella, Michael A.,Obermeier, Mary,Fura, Aberra,Chandrasena, Gamini
, p. 1910 - 1915 (2008/12/22)
A novel series of [2.2.1]-oxabicyclo imide-based compounds were identified as potent antagonists of the androgen receptor. Molecular modeling and iterative drug design were applied to optimize this series. The lead compound [3aS-(3aα,4β,5β,7β,7aα)]-4-(octahydro-5-hydroxy-4,7-dimethyl-1,3-dioxo-4,7-epoxy-2H-isoindol-2-yl)-2-iodobenzonitrile was shown to have potent in vivo efficacy after oral dosing in the CWR22 human prostate tumor xenograph model.
METHOD FOR THE PREPARATION OF FUSED HETEROCYCLIC SUCCINIMIDE COMPOUNDS AND ANALOGS THEREOF
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, (2008/06/13)
Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds.
Synthesis of novel iodo derived bicalutamide analogs
Nair, Vipin A.,Mustafa, Suni M.,Mohler, Michael L.,Fisher, Scott J.,Dalton, James T.,Miller, Duane D.
, p. 9475 - 9477 (2007/10/03)
A series of optically active nonsteroidal selective androgen receptor modulators with structures analogous to bicalutamide was prepared by replacing the trifluoromethyl group with iodine and the sulfonyl linker by oxygen.
Fused heterocyclic succinimide compounds and analogs thereof, modulators of nuclear hormone receptor function
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, (2008/06/13)
Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds.
Design, synthesis, and pharmacological characterization of 4-[4,4-Dimethyl-3-(4-hydroxybutyl)-5-oxo-2-thioxo-1-imidazolidinyl]-2-iodoben zonitrile as a high-affinity nonsteroidal androgen receptor ligand
Van Dort,Robins,Wayburn
, p. 3344 - 3347 (2007/10/03)
4-[4,4-Dimethyl-3-(4-hydroxybutyl)-5-oxo-2-thioxo-1-imidazolidinyl]-2-trifluo romethylbenzonitrile (RU 59063) is a prototype of a new class of high-affinity nonsteroidal androgen receptor (AR) ligands. The search for a radioiodinated AR ligand prompted us
