Design and synthesis of 4-[3,5-dioxo-11-oxa-4,9-diazatricyclo[5.3.1.0(2,6)]undec-4-yl]-2-trifluoromethyl- benzonitriles as androgen receptor antagonists.

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Xiao HY, Balog A, Attar RM, Fairfax D, Fleming LB, Holst CL, Martin GS, Rossiter LM, Chen J, Cvjic ME, Dell-John J, Geng J, Gottardis MM, Han WC, Nation A, Obermeier M, Rizzo CA, Schweizer L, Spires T Jr, Shan W, Gavai A, Salvati ME, Vite G

Design and synthesis of 4-[3,5-dioxo-11-oxa-4,9-diazatricyclo[5.3.1.0(2,6)]undec-4-yl]-2-trifluoromethyl- benzonitriles as androgen receptor antagonists.

Bioorg Med Chem Lett. 2010 Aug 1;20(15):4491-5. doi: 10.1016/j.bmcl.2010.06.034. Epub 2010 Jun 10.

PubMed ID

20584610 [ View in PubMed

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Abstract

A novel series of 4-[3,5-dioxo-11-oxa-4,9-diazatricyclo[5.3.1.0(2,6)]undec-4-yl]-2-trifluoromethyl- benzonitriles has been synthesized. The ability of these compounds to act as antagonists of the androgen receptor was investigated and several were found to have potent activity in vitro and in vivo.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Bicalutamide	Androgen receptor	IC 50 (nM)	400	N/A	N/A	Details
Bicalutamide	Androgen receptor	IC 50 (nM)	173	N/A	N/A	Details
Bicalutamide	Androgen receptor	Ki (nM)	64	N/A	N/A	Details