Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10595344 | Bioorganic & Medicinal Chemistry Letters | 2012 | 4 Pages |
Abstract
An extension of our previously reported 3,4-dihydroquinazoline derivative is investigated. Oral anti-tumoral activity of 3,4-dihydroquinazoline derivative (KYS05090) as potent and selective T-type calcium channel blocker was in vivo evaluated against A549 xenograft in BALB/cnu/nu nude mice. The rate of tumor volume increment in mouse model with KYS05090-treated group was remarkably slower than that of control group. With respect to tumor weight, it exhibited 60% and 67% tumor growth inhibition through oral administration of 1 and 5Â mg/kg of bodyweight, respectively, compared to control and was more potent than paclitaxel (53%). In addition, KYS05090 (10 and 50Â mg/kg, po) was found to have a marked analgesic effect in acetic acid-induced writhing test, whereas it did not show any effect on hot plate test.
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Authors
Han Byul Kang, Hong-Kun Rim, Jin Yeong Park, Heung Woo Choi, Doo Li Choi, Ji-Hyung Seo, Kyung-Sook Chung, Geun Huh, Jungahn Kim, Dong Joon Choo, Kyung-Tae Lee, Jae Yeol Lee,