Synthesis and Pharmacological Characterization of Disila-AM80 (Disila-tamibarotene) and Disila-AM580, Silicon Analogues of the RARα-Selective Retinoid Agonists AM80 (Tamibarotene) and AM580

Synthesis and Pharmacological Characterization of Disila-AM80 (Disila-tamibarotene) and Disila-AM580, Silicon Analogues of the RARα-Selective Retinoid Agonists AM80 (Tamibarotene) and AM580

C/Si switch: Twofold sila‐substitution (C/Si exchange) in the RARα‐selective retinoids 1 a (AM80) and 2 a (AM580) leads to 1 b (disila‐AM80) and 2 b (disila‐AM580), respectively. The chemistry and biology of the C/Si pairs are reported.

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Veröffentlicht in:ChemMedChem 2009-11, Vol.4 (11), p.1797-1802
Hauptverfasser: Tacke, Reinhold, Müller, Volker, Büttner, Matthias W., Lippert, W. Peter, Bertermann, Rüdiger, Daiß, Jürgen O., Khanwalkar, Harshal, Furst, Audrey, Gaudon, Claudine, Gronemeyer, Hinrich
Format: Artikel
Sprache:eng
Schlagworte:
bioinorganic chemistry
drugs
receptors
retinoid agonists
silicon
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Zusammenfassung:C/Si switch: Twofold sila‐substitution (C/Si exchange) in the RARα‐selective retinoids 1 a (AM80) and 2 a (AM580) leads to 1 b (disila‐AM80) and 2 b (disila‐AM580), respectively. The chemistry and biology of the C/Si pairs are reported.
ISSN:1860-7179
1860-7187
DOI:10.1002/cmdc.200900257