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Issue 12, 2016
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Identification of Gli-mediated transcription inhibitors through synthesis and evaluation of taepeenin D analogues

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Abstract

The Hedgehog pathway has emerged as a favourable target to address drug resistance in cancer stem cells. Inhibitors of Gli1, the terminal effector of the pathway, are anticipated to evade drug resistance and to display fewer side effects than inhibitors targeting Smo. Inspired by the Gli-mediated transcription inhibitor taepeenin D, synthesis and evaluation of a series of second generation analogues has led to the enrichment of available structure–activity relationships for this natural product and has identified an oxazole analogue as an improved lead compound.

Graphical abstract: Identification of Gli-mediated transcription inhibitors through synthesis and evaluation of taepeenin D analogues

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Publication details

The article was received on 25 Jun 2016, accepted on 08 Sep 2016 and first published on 15 Sep 2016


Article type: Research Article
DOI: 10.1039/C6MD00354K
Citation: Med. Chem. Commun., 2016,7, 2328-2331
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    Identification of Gli-mediated transcription inhibitors through synthesis and evaluation of taepeenin D analogues

    A. Antoniou, M. Chatzopoulou, M. Bantzi, C. M. Athanassopoulos, A. Giannis and E. N. Pitsinos, Med. Chem. Commun., 2016, 7, 2328
    DOI: 10.1039/C6MD00354K

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