title: Synthesis, cytotoxic activities and structure-activity relationships of topoisomerase I inhibitors: indolizinoquinoline-5,12-dione derivatives.
abstract: A series of indolizinoquinoline-5,12-dione derivatives (IQDs) are synthesized and evaluated for their cytotoxic activities toward human lung adenocarcinoma (GLC-82), large-cell lung carcinoma (NCI-H460), promyelocytic leukemia (HL-60) and breast carcinoma (MCF-7) cells by MTT method. Most of the IQDs show significant cytotoxic potency. In addition, the evaluation of structure-activity relationships indicated that the incorporation of electron-withdrawing substituents at the C or D ring will enhance the activities of the target compounds distinctly. The topoisomerase I inhibitory activity is also measured.
authors.affiliation: School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510080, China.
authors.forename: Yu
authors.initials: Y
authors.lastname: Cheng
authors.forename: Lin-Kun
authors.initials: LK
authors.lastname: An
authors.forename: Ning
authors.initials: N
authors.lastname: Wu
authors.forename: Xiao-Dong
authors.initials: XD
authors.lastname: Wang
authors.forename: Xian-Zhang
authors.initials: XZ
authors.lastname: Bu
authors.forename: Zhi-Shu
authors.initials: ZS
authors.lastname: Huang
authors.forename: Lian-Quan
authors.initials: LQ
authors.lastname: Gu
mesh_terms: D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004264:DNA Topoisomerases, Type I / Q000378:metabolism*; D004789:Enzyme Activation / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity*; D006801:Humans; D007211:Indoles / Q000737:chemistry*; D015394:Molecular Structure; D011804:Quinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity*; D013329:Structure-Activity Relationship; D059004:Topoisomerase I Inhibitors
chemical_list: D004791:Enzyme Inhibitors; D007211:Indoles; D011804:Quinolines; D059004:Topoisomerase I Inhibitors; C037219:quinoline; D004264:DNA Topoisomerases, Type I