title: In vivo evaluation of oral anti-tumoral effect of 3,4-dihydroquinazoline derivative on solid tumor.
abstract: An extension of our previously reported 3,4-dihydroquinazoline derivative is investigated. Oral anti-tumoral activity of 3,4-dihydroquinazoline derivative (KYS05090) as potent and selective T-type calcium channel blocker was in vivo evaluated against A549 xenograft in BALB/c(nu/nu) nude mice. The rate of tumor volume increment in mouse model with KYS05090-treated group was remarkably slower than that of control group. With respect to tumor weight, it exhibited 60% and 67% tumor growth inhibition through oral administration of 1 and 5mg/kg of bodyweight, respectively, compared to control and was more potent than paclitaxel (53%). In addition, KYS05090 (10 and 50mg/kg, po) was found to have a marked analgesic effect in acetic acid-induced writhing test, whereas it did not show any effect on hot plate test.
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: Han Byul
authors.initials: HB
authors.lastname: Kang
authors.forename: Hong-Kun
authors.initials: HK
authors.lastname: Rim
authors.forename: Jin Yeong
authors.initials: JY
authors.lastname: Park
authors.forename: Heung Woo
authors.initials: HW
authors.lastname: Choi
authors.forename: Doo Li
authors.initials: DL
authors.lastname: Choi
authors.forename: Ji-Hyung
authors.initials: JH
authors.lastname: Seo
authors.forename: Kyung-Sook
authors.initials: KS
authors.lastname: Chung
authors.forename: Geun
authors.initials: G
authors.lastname: Huh
authors.forename: Jungahn
authors.initials: J
authors.lastname: Kim
authors.forename: Dong Joon
authors.initials: DJ
authors.lastname: Choo
authors.forename: Kyung-Tae
authors.initials: KT
authors.lastname: Lee
authors.forename: Jae Yeol
authors.initials: JY
authors.lastname: Lee
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D006801:Humans; D051379:Mice; D008807:Mice, Inbred BALB C; D008813:Mice, Inbred ICR; D008819:Mice, Nude; D015394:Molecular Structure; D009369:Neoplasms / Q000188:drug therapy* / Q000473:pathology; D011799:Quinazolines / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D023041:Xenograft Model Antitumor Assays
chemical_list: D000970:Antineoplastic Agents; C549128:KYS 05090; D011799:Quinazolines