• 약학회지
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• 제49권4호
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• pp.335-339
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• 2005

In this study we investigated the effect of 3-methoxy-6-allylthiopyridazine on cell growth in BxPC3 and PANC1 human pancreatic cancer cells. The treatment with 3-methoxy-6-allylthiopyridazine for 48h decreased cell viability and induced apoptotic cell death in a dose-dependent manner, assessed by using the MTT assay and the flow cytometry, respectively. These results suggest that 3-methoxy-6-allylthiopyridazine may be a good candidate for the therapeutic management of human pancreatic cancers.

• 약학회지
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• 제44권1호
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• pp.9-15
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• 2000

Four 3-alkoxy-6-allylthiopyridazines and 3-chloro-6-allylthiopyridazine were synthesized and their protective effects against oxidative stress and UV-C irradiation were tested. 3-Methoxy-6-allylthiopyridazine and 3-ethoxy-6-allylthiopyridazine did not show protective effect on the oxidative stress but showed the strongest protective effect on UV-C irradiation among the tested compounds. Especially 500 $\mu\textrm{g}$/$m\ell$ of the two compounds was the most effective concentration.

• Biomolecules & Therapeutics
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• 제13권2호
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• pp.123-126
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• 2005

The single dose toxicity of 3-methoxy-6-allylthiopyridazine (K-6) was studied with Sprague-Dawley rats. K-6 was administered orally with dosages of 4.0, 3.0, 1.5, 1.0, 0.5, 0.25 and 0.1 g/kg to the rats. We observed daily the number of death, clinical signs, body weights and gross findings. All rats (6) were dead within a day after administration when doses of 4.0and 3.0 g/kg were administered. When dose of 2.0 g/kg was administered, 2 rats among 3 rats were dead. Any significant toxicity below 1.5g/kg of K6 was not observed when the different doses of 1.5, 1.0, 0.5, 0.25 and 0.1 g/kg were administered to 6 rats respectively.

• Archives of Pharmacal Research
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• 제26권5호
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• pp.351-357
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• 2003

Five kinds of allylthiopyridazine derivatives were synthesized and their chemoprotective activities examined in rats exposed to aflatoxin $B_1$-toxicant. Rats were pretreated with five allylthiopyridazine derivatives at daily oral doses of 50 mg/kg for 10 consecutive days, and during this period with one or three repeated doses of the potent hepatotoxin, aflatoxin $B_1$. The hepatoprotective effects of the allylthiopyridazine derivatives against aflatoxin $B_1$ (1 mg/kg, three times at intervals of 3 days, i.p., or at 3 mg/kg, once at final days, i.p.) administration were showed the significantly normal as compared with control in body and liver weights. Aspartate aminotransferase and alanine aminotransferase levels were markedly elevated after aflatoxin $B_1$ administration, and pretreatment with allylthiopyridazine derivatives, before aflatoxin $B_1$ administration, resulted in decreased levels of these enzymes. In addition, the allylthiopyridazine derivatives, K6 (3-methoxy-), K8 (3-chloro-), K16 (3-ethoxy-) and K17 (3-n-propoxy), induced elevated hepatic GSH levels. Four kinds of allylthiopyridazine derivatives investigated were effective against aflatoxin $B_1$ -induced hepatotoxicity.