title: Synthesis and antitumor activity of conjugates of 5-Fluorouracil and emodin.
abstract: A series of conjugates of 5-Fluorouracil (5-FU) and emodin were synthesized by coupling trimethyl emodin with N(1), N(3) dialkylated 5-FU. The 5-FU moiety contained various substituents at the N(3)-position were linked to the 2-position of trimethyl emodin via a methylene linkage. Their cytotoxicity against three cancer cell lines and one noncancerous cell were studied. The results revealed that some of conjugates exhibited better or comparable in vitro antitumor activity to 5-FU and emodin and low toxicity in the normal cell. The structure-activity relationship study showed N(3)-aromatic substituent was important for their cytotoxic activity.
authors.affiliation: School of Chemistry and Chemical Engineering, Xuzhou Normal University, Xuzhou 221116, Jiangsu, China. lmzhao@xznu.edu.cn
authors.forename: Li-Ming
authors.initials: LM
authors.lastname: Zhao
authors.forename: Li-Ming
authors.initials: LM
authors.lastname: Zhang
authors.forename: Jin-Juan
authors.initials: JJ
authors.lastname: Liu
authors.forename: Li-Jing
authors.initials: LJ
authors.lastname: Wan
authors.forename: Yong-Qiang
authors.initials: YQ
authors.lastname: Chen
authors.forename: Shu-Qing
authors.initials: SQ
authors.lastname: Zhang
authors.forename: Zhi-Wei
authors.initials: ZW
authors.lastname: Yan
authors.forename: Ji-Hong
authors.initials: JH
authors.lastname: Jiang
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004642:Emodin / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D005472:Fluorouracil / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D006801:Humans; D020128:Inhibitory Concentration 50
chemical_list: D000970:Antineoplastic Agents; D004642:Emodin; D005472:Fluorouracil