2. Academic Validation
  3. Pyridazinopsoralens of wide chemotherapeutic interest

Pyridazinopsoralens of wide chemotherapeutic interest

  • Bioorg Med Chem. 2010 Aug 1;18(15):5708-14. doi: 10.1016/j.bmc.2010.06.006.
Lisa Dalla Via 1,  Ornella Gia,  Sebastiano Marciani Magno,  Alessandra Braga,  José Carlos González-Gómez,  Lázaro Guillermo Pérez-Montoto,  Eugenio Uriarte
Affiliations

Affiliation

  • 1 Department of Pharmaceutical Sciences, University of Padova, Via F Marzolo 5, I-35131 Padova, Italy. lisa.dallavia@unipd.it
PMID: 20615713 DOI: 10.1016/j.bmc.2010.06.006
Abstract

The synthesis of new 6,10-dimethylpyridazino[4,5-h]psoralens, carrying no (4), one (5), or two (6-9) dialkylaminoalkylcarboxamide side chains on the pyridazine ring is reported. All compounds exert a significant photoantiproliferative activity. Moreover, the derivatives characterised by the protonable side chains show a notable cytotoxicity in the dark. The investigation on the mechanism of action demonstrated the capacity to intercalate into DNA base pairs and to inhibit the relaxation activity of Topoisomerase II.

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