title: Synthesis and biological evaluation of novel indoline-2,3-dione derivatives as antitumor agents.
abstract: A new series of 1,5-disubstituted indolin-2,3-diones was synthesized and their inhibition of the growth of a human acute promyelocytic leukemia (HL-60) cell line was evaluated. These compounds had promising inhibition of HL-60 cell growth in vitro. Results indicated that compounds with a benzyl substituent at the N-1 position on the indolin-2,3-dione ring had more potent antiproliferative activity than those with a (4-fluorobenzyl) amino-2-oxoethyl substituent at the N-1 position. Among the compounds synthesized, compound 8l inhibited half of cell growth at a concentration of 0.07 μM and compound 8p did so at a concentration of 0.14 μM. These compounds may serve as lead compounds for further optimization in order to develop novel anticancer agents.
authors.affiliation: Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University.
authors.forename: Pengzhan
authors.initials: P
authors.lastname: Li
authors.forename: Yanmei
authors.initials: Y
authors.lastname: Tan
authors.forename: Guyue
authors.initials: G
authors.lastname: Liu
authors.forename: Yang
authors.initials: Y
authors.lastname: Liu
authors.forename: Jianzhen
authors.initials: J
authors.lastname: Liu
authors.forename: Yanzhen
authors.initials: Y
authors.lastname: Yin
authors.forename: Guisen
authors.initials: G
authors.lastname: Zhao
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D018922:HL-60 Cells; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D007211:Indoles; C572590:indoline-2,3-dione