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http://dx.doi.org/10.5012/bkcs.2013.34.2.482

Evaluation of T-Type Calcium Channel Blockers against Human Pancreatic MIA PaCa-2 Carcinoma Xenografts  

Park, Jin Yeong (Research Institute for Basic Sciences and Department of Chemistry, College of Sciences, Kyung Hee University)
Choi, Heung Woo (Research Institute for Basic Sciences and Department of Chemistry, College of Sciences, Kyung Hee University)
Choi, Doo Li (Research Institute for Basic Sciences and Department of Chemistry, College of Sciences, Kyung Hee University)
Jang, Sun Jeong (Research Institute for Basic Sciences and Department of Chemistry, College of Sciences, Kyung Hee University)
Kim, Je Hak (Central Research Institute, Boryung Pharm. Co. Ltd.)
Lee, Joo Han (Central Research Institute, Boryung Pharm. Co. Ltd.)
Choo, Dong Joon (Research Institute for Basic Sciences and Department of Chemistry, College of Sciences, Kyung Hee University)
Kim, Jungahn (Research Institute for Basic Sciences and Department of Chemistry, College of Sciences, Kyung Hee University)
Lee, Kyung-Tae (Department of Pharmaceutical Biochemistry, College of Pharmacy, Kyung Hee University)
Lee, Jae Yeol (Research Institute for Basic Sciences and Department of Chemistry, College of Sciences, Kyung Hee University)
Publication Information
Bulletin of the Korean Chemical Society / v.34, no.2, 2013 , pp. 482-488 More about this Journal
Abstract
Two piperazine-containing 3,4-dihyroquinazolines (BK10007S/8S) have been synthesized, based on our previous work on the synthesis and antitumoral activity of 3,4-dihyroquinazolines. After evaluating them for T-type calcium channel blocking effect and in vitro anti-cancer effect, they were profiled for acute and repeat dose toxicity (40 mg/kg, 2 weeks) to BALB/c mice. BK10007S/8S were further in vivo evaluated against human pancreatic MIA PaCa-2 carcinoma in $BALB/c^{nu/nu}$ nude mice, which exhibited 54 and 61% tumor growth inhibition through 57-day oral administration of 2 mg/kg of body weight, respectively.
Keywords
T-type calcium channel; 3,4-Dihydroquinazoline; Repeat dose toxicity; MIA PaCa-2 xenografts;
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