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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 34, Number 2
BKCSDE 34(2)
February 20, 2013 

Evaluation of T-Type Calcium Channel Blockers against Human Pancreatic MIA PaCa-2 Carcinoma Xenografts
Jin Yeong Park, Heung Woo Choi, Doo Li Choi, Sun Jeong Jang, Je Hak Kim, Joo Han Lee, Dong Joon Choo, Jungahn Kim, Kyung-Tae Lee, Jae Yeol Lee*
T-type calcium channel, 3,4-Dihydroquinazoline, Repeat dose toxicity, MIA PaCa-2 xenografts
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/cnu/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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