Alliums is known to have anticancer and antihypertensive effects. One of the Alliums plants reported to possess antitumor compounds was garlic, used for treatment of tumors by ancient civilizations. The allyl sulfides were found in garlic may play a key role in its an pharmacophore and their cytotoxicity was experimented in previous study. Organoseleniums have reported an antioxidant, an enzyme inhibitor, a neuroprotective agent, an anticancer agent in pharmacological studies. The results of the drug design, 3-allylseleno-6-substituted pyridazine derivatives were expected to retain anticancer activity. In this study, the synthetic route for the target organoselenium pyridazines was proceeded via alkylthiolation, oxidation, diselenylation, hydrolysis and Se-allylation from 3,6-dichloropyridazine. The core compounds, disulfoxide(or sulfonyl)pyridazinyl diselenide, were prepared from the diselenide anion of Na2Se2 and the alkylsulfoxide(or sulfonyl)pyridazinyl chloride by the synthetic route of Bhasin. Finally, target 3-allylselenopyridazine derivatives can be synthesized from the disulfoxide(or sulfonyl)pyridazinyl diselenide with allyl bromide. The synthetic compounds were investigated to antitumor effect against human colon carcinoma Hep3B and human breast cancer MCF-7 cells. We evaluated the cytotoxic activities of the newly synthesized compounds against cancer cell line in CCK-8 assay.

Transformations of allicin from garlic: The discovery of allylselenoalkylsulfonylpyridazines and Its antitumor activity

249th National Meeting (2015)

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.