Antitumor activity of 3,4-dihydroquinazoline dihydrochloride in A549 xenograft nude mice.
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.
Jung
Soo Yeon
SY
Research Institute for Basic Sciences and Department of Chemistry, College of Sciences, Kyung Hee University, Seoul 130-701, Republic of Korea.
Lee
So Hyung
SH
Kang
Han Byul
HB
Park
Hang Ah
HA
Chang
Sun Ki
SK
Kim
Jungahn
J
Choo
Dong Joon
DJ
Oh
Chun Rim
CR
Kim
Young Deuk
YD
Seo
Ji Hyung
JH
Lee
Kyung-Tae
KT
Lee
Jae Yeol
JY
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
C556784:3,4-dihydroquinazoline dihydrochloride; D000970:Antineoplastic Agents; D011799:Quinazolines