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Bioorg Med Chem Lett ; 20(22): 6633-6, 2010 Nov 15.
Article in English | MEDLINE | ID: mdl-20884207

ABSTRACT

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 LD(50) values of 693 mg/kg (p.o. route) and 40.0 mg/kg (i.v. route) of body weight. In addition, its efficient scale-up synthetic method was developed.


Subject(s)
Antineoplastic Agents/pharmacology , Quinazolines/pharmacology , Animals , Cell Line, Tumor , Drug Screening Assays, Antitumor , Humans , Lethal Dose 50 , Mice , Mice, Inbred BALB C , Mice, Nude , Transplantation, Heterologous
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