title: Synthesis and cytotoxicity of 2-phenylquinazolin-4(3H)-one derivatives.
abstract: Thirty 2-phenylquinazolin-4(3H)-one derivatives were prepared and their cytotoxic activities were tested in five human tumor cell lines. Some compounds (5e, 5k, 5t, 6c and 6f) showed relatively high cytotoxic activity. Especially, compound 6c showed the most cytotoxicity against all cell lines tested among the synthesized derivatives, and the inhibitory activity of 6c against HeLa cell was higher than that of adriamycin. The putative mechanism of antitumor action in apoptotic cell death was cell cycle arrest in the G0/G1 phase by compounds 5k, 5v, 5m, 6c, and 6f in HeLa cells. These compounds showed relatively high cytotoxicity in this cell type.
authors.affiliation: College of Pharmacy & Division of Life & Pharmaceutical Sciences, Ewha Womans University, Seoul 120-750, Korea.
authors.forename: Hee-Kyung
authors.initials: HK
authors.lastname: Rhee
authors.forename: Ji Hye
authors.initials: JH
authors.lastname: Yoo
authors.forename: Eunyoung
authors.initials: E
authors.lastname: Lee
authors.forename: Young Joo
authors.initials: YJ
authors.lastname: Kwon
authors.forename: Hang-Rhan
authors.initials: HR
authors.lastname: Seo
authors.forename: Yun-Sil
authors.initials: YS
authors.lastname: Lee
authors.forename: Hea-Young Park
authors.initials: HY
authors.lastname: Choo
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis; D002453:Cell Cycle; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D011799:Quinazolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D016339:Spectrometry, Mass, Fast Atom Bombardment; D013055:Spectrophotometry, Infrared; D013329:Structure-Activity Relationship
chemical_list: C516488:2-phenylquinazoline; D000970:Antineoplastic Agents; D011799:Quinazolines