Quinol-4-ones as steroid A-ring mimetics in nonsteroidal dissociated glucocorticoid agonists.

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Regan J, Lee TW, Zindell RM, Bekkali Y, Bentzien J, Gilmore T, Hammach A, Kirrane TM, Kukulka AJ, Kuzmich D, Nelson RM, Proudfoot JR, Ralph M, Pelletier J, Souza D, Zuvela-Jelaska L, Nabozny G, Thomson DS

Quinol-4-ones as steroid A-ring mimetics in nonsteroidal dissociated glucocorticoid agonists.

J Med Chem. 2006 Dec 28;49(26):7887-96.

PubMed ID

17181172 [ View in PubMed

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Abstract

We report on the nuclear receptor binding affinities, cellular activities of transrepression and transactivation, and anti-inflammatory properties of a quinol-4-one and other A-ring mimetic containing nonsteroidal class of glucocorticoid agonists.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Dexamethasone	Glucocorticoid receptor	IC 50 (nM)	3	N/A	N/A	Details
Prednisolone	Glucocorticoid receptor	IC 50 (nM)	15	N/A	N/A	Details