5(Z)-benzylidene-1,2-dihydro-9-hydroxy-10-methoxy-2,2,4-trimethyl-5H-1-aza-6-oxa- chrysenes as non-steroidal glucocorticoid receptor modulators.

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Ardecky RJ, Hudson AR, Phillips DP, Tyhonas JS, Deckhut C, Lau TL, Li Y, Martinborough EA, Roach SL, Higuchi RI, Lopez FJ, Marschke KB, Miner JN, Karanewsky DS, Negro-Vilar A, Zhi L

5(Z)-benzylidene-1,2-dihydro-9-hydroxy-10-methoxy-2,2,4-trimethyl-5H-1-aza-6-oxa- chrysenes as non-steroidal glucocorticoid receptor modulators.

Bioorg Med Chem Lett. 2007 Aug 1;17(15):4158-62. Epub 2007 May 23.

PubMed ID

17553679 [ View in PubMed

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Abstract

A series of 5-benzylidene-1,2-dihydro-2,2,4-trimethyl-5H-1-aza-6-oxa-chrysenes was synthesized and profiled for their ability to act as selective glucocorticoid receptor modulators (SGRMs). The synthesis and structure-activity relationships for this series of compounds are presented.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Prednisolone	Glucocorticoid receptor	IC 50 (nM)	>1000	N/A	N/A	Details
Prednisolone	Glucocorticoid receptor	EC 50 (nM)	5.3	N/A	N/A	Details
Prednisolone	Glucocorticoid receptor	Ki (nM)	5.3	N/A	N/A	Details
Prednisolone	Glucocorticoid receptor	IC 50 (nM)	4.1	N/A	N/A	Details