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Issue 15, 2009
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Synthesis and biological evaluation of functionalised tetrahydro-β-carboline analogues as inhibitors of Toxoplasma gondii invasion

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Abstract

Techniques for the identification of the protein target(s) of small molecules are proving very important following an increase in the use of phenotype-based screening in chemical biology and drug discovery. One approach, known as the yeast-3-hybrid approach, has shown considerable potential. A key factor in the success of this approach is the preparation of a complex molecule referred to as a chemical inducer of dimerisation (CID). The synthesis of two CIDs based on a bioactive tetrahydro-β-carboline core structure is reported and evidence presented that shows the CIDs are of utility in this approach. A series of chemo- and bioinformatic studies coupled with SAR development inspired the choice of CIDs.

Graphical abstract: Synthesis and biological evaluation of functionalised tetrahydro-β-carboline analogues as inhibitors of Toxoplasma gondii invasion

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Publication details

The article was received on 04 Feb 2009, accepted on 22 May 2009 and first published on 17 Jun 2009


Article type: Paper
DOI: 10.1039/B902319D
Citation: Org. Biomol. Chem., 2009,7, 3049-3060
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    Synthesis and biological evaluation of functionalised tetrahydro-β-carboline analogues as inhibitors of Toxoplasma gondii invasion

    J. G. A. Walton, S. Patterson, G. Liu, J. D. Haraldsen, J. J. Hollick, A. M. Z. Slawin, G. E. Ward and N. J. Westwood, Org. Biomol. Chem., 2009, 7, 3049
    DOI: 10.1039/B902319D

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