2. Academic Validation
  3. 3,4-Dihydro-1H-[1,3]oxazino[4,5-c]acridines as a new family of cytotoxic drugs

3,4-Dihydro-1H-[1,3]oxazino[4,5-c]acridines as a new family of cytotoxic drugs

  • Bioorg Med Chem Lett. 2006 Sep 1;16(17):4641-3. doi: 10.1016/j.bmcl.2006.05.101.
Myriam Ouberai 1,  Christian Asche,  Danièle Carrez,  Alain Croisy,  Pascal Dumy,  Martine Demeunynck
Affiliations

Affiliation

  • 1 LEDSS, CNRS UMR 5616 & ICMG-FR260, Université Joseph Fourier, BP53, Grenoble, France.
PMID: 16777412 DOI: 10.1016/j.bmcl.2006.05.101
Abstract

A series of [1,3]oxazino fused acridines has been prepared as precursors of cytotoxic 3-amino-4-hydroxymethylacridine 2. Their cytotoxic activity has been evaluated against HT29 colon carcinoma cell line and was shown to be dependent on the nature of the substituent located on position 2 of the oxazine ring. Additionally, the nitrophenyl derivative 3f is activated by nitroreductase, indicating its potency as prodrug for either gene-directed or antibody-directed enzyme prodrug therapies.

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