☆ 4.6 Article

Synthesis and biological evaluation of functionalised tetrahydro-beta-carboline analogues as inhibitors of Toxoplasma gondii invasion

ORGANIC & BIOMOLECULAR CHEMISTRY (2009)

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ORGANIC & BIOMOLECULAR CHEMISTRY
Volume 7, Issue 15, Pages 3049-3060

Publisher

ROYAL SOC CHEMISTRY
DOI: 10.1039/b902319d

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Categories

Chemistry, Organic

Funding

  1. PHS [AI054961]
  2. Royal Society (NJW URF Fellowship)

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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-beta-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.

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