title: Synthesis and cytotoxic activities of 2-alkyl-2,3-dihydro-1H-2,6,9-triazacyclopenta[b]anthracene-5,10-diones.
abstract: A series of 2-alkyl-2,3-dihydro-1H-2,6,9-triazacyclopenta[b]anthracene-5,10-diones (4a-f) were synthesized and their in vitro cytotoxic activities were evaluated against six human cancer cell lines (HCT15, SK-OV-3, A549, SNB19, MCF7 and MCF7/ADR). A number of compounds including 4c and 4d showed 2-180 times more potent cytotoxic activity than doxorubicin against all human cancer cell lines tested. Furthermore, these compounds retained considerable cytotoxic activity against the doxorubicin-resistant cell line MCF7/ADR, implying their therapeutic potential to treat doxorubicin-resistant tumors.
authors.affiliation: College of Pharmacy, Chungbuk National University, Cheongju 361-763, Korea.
authors.forename: Jae-Hwan
authors.initials: JH
authors.lastname: Kwak
authors.forename: Kwon
authors.initials: K
authors.lastname: Namgoong
authors.forename: Jae-Kyung
authors.initials: JK
authors.lastname: Jung
authors.forename: Jungsook
authors.initials: J
authors.lastname: Cho
authors.forename: Hwan-Mook
authors.initials: HM
authors.lastname: Kim
authors.forename: Sung-Gyu
authors.initials: SG
authors.lastname: Park
authors.forename: Yeong-Ah
authors.initials: YA
authors.lastname: Yoo
authors.forename: Joo-Hee
authors.initials: JH
authors.lastname: Kwon
authors.forename: Heesoon
authors.initials: H
authors.lastname: Lee
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D011719:Pyrazines / Q000138:chemical synthesis* / Q000494:pharmacology*; D011809:Quinones / Q000138:chemical synthesis* / Q000494:pharmacology*; D012235:Rhodamines; D013055:Spectrophotometry, Infrared; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D011719:Pyrazines; D011809:Quinones; D012235:Rhodamines; C022027:lissamine rhodamine B