کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1371620 981849 2010 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Antitumor activity of 3,4-dihydroquinazoline dihydrochloride in A549 xenograft nude mice
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Antitumor activity of 3,4-dihydroquinazoline dihydrochloride in A549 xenograft nude mice
چکیده انگلیسی

In the previous article we have reported that 3,4-dihydroquinazoline 1 is a potent and selective T-type calcium channel blocker that exhibited strong anti-cancer activity in vitro. Compound 1·2HCl was further in vivo evaluated against A549 xenograft in BALB/c nude mice, which exhibited 49% tumor-weight inhibition through intravenous administration of 2 mg/kg of body weight and was more potent than doxorubicin. Moreover, compound 1·2HCl has an oral bioavailability of 98% with LD50 values of 693 mg/kg (po route) and 40.0 mg/kg (iv route) of body weight. In addition, its efficient scale-up synthetic method was developed.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 22, 15 November 2010, Pages 6633–6636
نویسندگان
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