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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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Supplementary files

Article information


Submitted
04 Feb 2009
Accepted
22 May 2009
First published
17 Jun 2009

Org. Biomol. Chem., 2009,7, 3049-3060
Article type
Paper

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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