title: Selenium-containing naphthalimides as anticancer agents: design, synthesis and bioactivity.
abstract: Selenium analogues (4b-4h, and 4j) of two known sulfur compounds were synthesized and tested their anticancer activities. The selenium compound 4b had comparable activity with its sulfur analogue 4a, while DNA-binding study showed these two compounds had similar interaction with ct-DNA, the K(b) was 8.23 and 2.36, respectively. The primary results showed that most compounds had moderate anticancer activities with IC(50) values between 10(-6) and 10(-5) M. Another selenium analogue 4j showed the highest activity with the IC(50) values around 5.3 μM against K562 and MCF-7 cell lines. More importantly, the organochalcogen compounds exhibited stronger anticancer activities against K562 cell line than the other cell lines tested.
authors.affiliation: Shanghai Key Lab of Chemical Biology, School of Pharmacy, East China University of Science and Technology, Meilong Road 130, Shanghai 200237, China.
authors.forename: Liwei
authors.initials: L
authors.lastname: Zhao
authors.forename: Jianfeng
authors.initials: J
authors.lastname: Li
authors.forename: Yiquan
authors.initials: Y
authors.lastname: Li
authors.forename: Jianwen
authors.initials: J
authors.lastname: Liu
authors.forename: Thomas
authors.initials: T
authors.lastname: Wirth
authors.forename: Zhong
authors.initials: Z
authors.lastname: Li
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002417:Cattle; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004247:DNA / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D006367:HeLa Cells; D006801:Humans; D020014:K562 Cells; D015394:Molecular Structure; D053644:Naphthalimides / Q000737:chemistry*; D009942:Organometallic Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D012643:Selenium / Q000737:chemistry*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D053644:Naphthalimides; D009942:Organometallic Compounds; D004247:DNA; C427203:calf thymus DNA; D012643:Selenium