Design, synthesis and evaluation of bouvardin, deoxybouvardin and RA-I-XIV pharmacophore analogs

Academic Article
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publication date

  • 1994

abstract

  • The synthesis and in vitro cytotoxic evaluation of a key set of cycloisodityrosine subunit analogs of deoxybouvardin and RA-VII are detailed and constitute a complete investigation of the natural product pharmacophore. The studies illustrate that the 18-membered ring tetrapeptide potentiation of the cytotoxic activity of cycloisodityrosine is not likely to be due to simple alteration or constraint of the conformation of the 14-membered cycloisodityrosine subunit and that simple derivatization of cycloisodityrosine may not provide the same potentiation.