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Microwave-Assisted Preparation of 1-Aryl-1H-pyrazole-5-amines
Published on: June 23, 2019
Pyridazinopsoralens of wide chemotherapeutic interest
Lisa Dalla Via1, Ornella Gia, Sebastiano Marciani Magno
1Department of Pharmaceutical Sciences, University of Padova, Via F Marzolo 5, I-35131 Padova, Italy. lisa.dallavia@unipd.it
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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