Bulletin of the Korean Chemical Society

Korean Chemical Society (대한화학회)
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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)
  • Received : 2012.10.31
  • Accepted : 2012.11.19
  • Published : 2013.02.20
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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.

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