84507-68-6Relevant articles and documents
Stereoselective synthesis and moulting activity of 2,3-diepi-20- hydroxyecdysone and 2,3-diepi-5α-20-hydroxyecdysone
Homvisasevongsa, Sureeporn,Chuaynugul, Aporn,Chimnoi, Nitirat,Suksamrarn, Apichart
, p. 3433 - 3438 (2004)
The ecdysteroid analogues 2,3-diepi-20-hydroxyecdysone and 2,3-diepi-5α-20-hydroxyecdysone have been synthesized from the readily available ecdysteroid, 20-hydroxyecdysone, and moulting activity has been determined using the Musca bioassay. As expected, the 2,3-diepi-analogue was less active than the parent ecdysteroid, 20-hydroxyecdysone. However, the 2,3-diepi-5α-analogue, which was expected to be inactive in the assay, exhibited moulting activity though it was approximately 1.5-fold less active than its 5β-analogue. The activity of the 5α-analogue could possibly result from the ability of this compound to bind to the ecdysteroid receptor. Alternatively, a possible in vivo C-5 epimerization of the 2,3-diepi-5α- analogue to the corresponding 5β-analogue could account for its activity.
Steroidal ligands and their use in gene switch modulation
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Page/Page column 46, (2016/02/15)
The present invention relates to steroidal ligands for use in nuclear receptor-based inducible gene expression systems. The invention further relates to methods of modulating the expression of genes of interest with a system containing one or more nuclear
Synthesis and structure-activity relationships of novel ecdysteroid dioxolanes as MDR modulators in cancer
Martins, Ana,Csabi, Jozsef,Balazs, Attila,Kitka, Diana,Amaral, Leonard,Molnar, Jozsef,Simon, Andras,Toth, Gabor,Hunyadi, Attila
, p. 15255 - 15275 (2014/01/17)
Ecdysteroids, molting hormones of insects, can exert several mild, non-hormonal bioactivities in mammals, including humans. In a previous study, we have found a significant effect of certain derivatives on the ABCB1 transporter mediated multi-drug resistance of a transfected murine leukemia cell line. In this paper, we present a structure-activity relationship study focused on the apolar dioxolane derivatives of 20-hydroxyecdysone. Semi-synthesis and bioactivity of a total of 32 ecdysteroids, including 20 new compounds, is presented, supplemented with their complete 1H- and 13C-NMR signal assignment.