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

被引：6

作者：

Park, Jin Yeong ^{[1
,2
]}

Choi, Heung Woo ^{[1
,2
]}

Choi, Doo Li ^{[1
,2
]}

Jang, Sun Jeong ^{[1
,2
]}

Kim, Je Hak ^{[3
]}

Lee, Joo Han ^{[2
,3
]}

Choo, Doug Joon ^{[1
,2
]}

Kim, Jungahn ^{[1
]}

Lee, Kyung-Tae ^{[4
]}

Lee, Jae Yeol ^{[1
,2
]}

机构：

[1] Kyung Hee Univ, Coll Sci, Res Inst Basic Sci, Seoul 130701, South Korea

[2] Kyung Hee Univ, Coll Sci, Dept Chem, Seoul 130701, South Korea

[3] Boryung Pharm Co Ltd, Cent Res Inst, Kyonggi Do 425839, South Korea

[4] Kyung Hee Univ, Coll Pharm, Dept Pharmaceut Biochem, Seoul 130701, South Korea

来源：

BULLETIN OF THE KOREAN CHEMICAL SOCIETY | 2013年 / 34卷 / 02期

基金：

新加坡国家研究基金会;

关键词：

T-type calcium channel; 3,4-Dihydroquinazoline; Repeat dose toxicity; MIA PaCa-2 xenografts; CANCER-CELLS; IN-VIVO; TUMOR; GROWTH; DIFFERENTIATION; PROLIFERATION; MICE;

D O I：

10.5012/bkcs.2013.34.2.482

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

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.

引用

页码：482 / 488

页数：7

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