Antitumour imidazotetrazines. Part 37. Conjugation of the DNA major-groove alkylating imidazotetrazine mitozolomide to peptide motifs recognizing the minor groove.

@article{Arrowsmith1999AntitumourIP,
  title={Antitumour imidazotetrazines. Part 37. Conjugation of the DNA major-groove alkylating imidazotetrazine mitozolomide to peptide motifs recognizing the minor groove.},
  author={Jill Arrowsmith and Sotiris Missailidis and Malcolm F. G. Stevens},
  journal={Anti-cancer drug design},
  year={1999},
  volume={14 3},
  pages={205-17}
}
Methods have been developed to conjugate the antitumour imidazotetrazines mitozolomide and temozolomide to DNA minor and major groove-binding peptidic motifs by solid phase peptide synthesis. Side chain deprotection and resin cleavage steps were accomplished under acidic conditions to maintain the structural integrity of the imidazotetrazine nucleus. When mitozolomide was conjugated to the DNA minor groove-binding peptide (SPKK)2-NH2 (3) a strong preference for binding with [dA-dT]2 sequences… CONTINUE READING

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