Synthesis and pharmacological characterization of Disila-AM80 (Disilatamibarotene) and Disila-AM580, silicon analogues of the RARΑ-selective retinoid agonists AM80 (Tamibarotene) and AM580

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Abstract

C/Si switch: Twofold sila-substitution (C/Si exchange) in the RARa-selective retinoids 1a (AM80) and 2a (AM580) leads to 1b (disila-AM80) and 2b (disila-AM580), respectively. The chemistry and biology of the C/Si pairs are reported. (Chemical Equation Presented) © 2009 Wiley-VCH Verlag GmbH & Co. KGaA.

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Tacke, R., Müller, V., Büttner, M. W., Lippert, W. P., Bertermann, R., Daiß, J. O., … Gronemeyer, H. (2009). Synthesis and pharmacological characterization of Disila-AM80 (Disilatamibarotene) and Disila-AM580, silicon analogues of the RARΑ-selective retinoid agonists AM80 (Tamibarotene) and AM580. ChemMedChem, 4(11), 1797–1802. https://doi.org/10.1002/cmdc.200900257

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