• 대한약학회:학술대회논문집
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• 대한약학회 2000년도 NEW STRATEGY FOR DRUG DEVELOPMENT IN POST-GENOMIC ERA(대한약학회)
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• pp.182.3-183
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• 2000

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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• pp.218.1-218.1
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• 2003

Dietary organosulfur compounds have been shown to inhibit the proliferation of tumor cells. Synthetic sulfur-containing compounds including oltipraz exert chemopreventive and hepatoprotective effects. We previously showed that synthetic allylthiopyridazine derivatives designated as K compounds induced apoptosis in SK-Hep-1 hepatocarcinoma cells (Eur. J. Cancer: 37, 2104-10, 2001). (omitted)

• 약학회지
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• 제55권1호
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• pp.32-38
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• 2011

A series of new alkylselenoallylthiopyridazine 12~18 was synthesized as expected to retain anticancer activity. Synthetic route for the final compounds 12~18 was proceeded with diselenylation, hydrolysis/alkylation and allylthiolation from 3,6-dichloropyridazine 1. Dichloropyridazinyl diselenide 2 was prepared from the diselenide anion using synthetic route of Bhasin. Diselenide 2 can be reduced to 3-chloropyridazinyl selenolate anion using hydrazine hydrate at rt in the presence of NaOH in THF. The anion thus formed reacts readily with alkyl halide to give the 3-alkylseleno-6-chloropyridazine 3~11. 3-Alkylseleno-6-allylthiopyridazines 12~18 were prepared from 3~11 with allylmercaptan and sodium methoxide.

• 약학회지
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• 제49권6호
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• pp.505-510
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• 2005

Allylthio group of allicin and other organosulfur compounds which are isolated from garlic is considered as a pharmacophore, a key structure component of the molecule which is responsible biological activities. In the foregoing studies various 3-allylthio -6- alkoxypyridazine derivatives (K- compounds ) and 3-allylthio -6- alkylthiopyridazine derivatives(Thio-K-compounds) were synthesized and their biological activities were tested in vivo. They showed good hepatoprotective activities on the carbon tetrachloride-treated mouse and aflatoxin Bl-treated rat and chemopreventive activities on bepatocarcinoma cells in rat as expected. Now 3-allylthio-6-heterocyclylalkylaminopyridazine derivatives that the oxygen atom at 6-Position of 3-allylthio-6-alkoxypyridazine is replaced by nitrogen (N) were synthesiz ed and their activities were tested in vitro against SK-Hep-1 human liver cancer cells. They showed good chemopreventive activities on hepatocarcinoma cells.