Steroidal C-21 mercapto derivatives as dissociated steroids: discovery of an inhaled dissociated steroid.

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Biju P, McCormick K, Aslanian R, Berlin M, Solomon D, Chapman R, McLeod R, Prelusky D, Eckel S, Kelly G, Natiello M, House A, Fernandez X, Bitar R, Phillips J, Anthes J

Steroidal C-21 mercapto derivatives as dissociated steroids: discovery of an inhaled dissociated steroid.

Bioorg Med Chem Lett. 2011 Nov 1;21(21):6343-7. doi: 10.1016/j.bmcl.2011.08.108. Epub 2011 Aug 31.

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21944381 [View in PubMed

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Abstract

A series of C-21 mercapto derivatives of hydrocortisone have been synthesized and evaluated in cell based transrepression and transactivation assays. The benzothiazole derivative, compound 6 not only showed a dissociated profile in vitro functional assays but also a pharmacological profile in a Brown-Norway rat therapeutic index model of asthma that dissociated side effects (thymolysis) while maintaining efficacy against pulmonary inflammation and lung function.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Fluticasone propionate	Glucocorticoid receptor	EC 50 (nM)	0.7	N/A	N/A	Details
Fluticasone propionate	Glucocorticoid receptor	IC 50 (nM)	0.075	N/A	N/A	Details