title: Antitumor activity of 3,4-dihydroquinazoline dihydrochloride in A549 xenograft nude mice.
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.
authors.affiliation: Research Institute for Basic Sciences and Department of Chemistry, College of Sciences, Kyung Hee University, Seoul 130-701, Republic of Korea.
authors.forename: Soo Yeon
authors.initials: SY
authors.lastname: Jung
authors.forename: So Hyung
authors.initials: SH
authors.lastname: Lee
authors.forename: Han Byul
authors.initials: HB
authors.lastname: Kang
authors.forename: Hang Ah
authors.initials: HA
authors.lastname: Park
authors.forename: Sun Ki
authors.initials: SK
authors.lastname: Chang
authors.forename: Jungahn
authors.initials: J
authors.lastname: Kim
authors.forename: Dong Joon
authors.initials: DJ
authors.lastname: Choo
authors.forename: Chun Rim
authors.initials: CR
authors.lastname: Oh
authors.forename: Young Deuk
authors.initials: YD
authors.lastname: Kim
authors.forename: Ji Hyung
authors.initials: JH
authors.lastname: Seo
authors.forename: Kyung-Tae
authors.initials: KT
authors.lastname: Lee
authors.forename: Jae Yeol
authors.initials: JY
authors.lastname: Lee
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D007928:Lethal Dose 50; D051379:Mice; D008807:Mice, Inbred BALB C; D008819:Mice, Nude; D011799:Quinazolines / Q000494:pharmacology*; D014183:Transplantation, Heterologous
chemical_list: C556784:3,4-dihydroquinazoline dihydrochloride; D000970:Antineoplastic Agents; D011799:Quinazolines