title: Synthesis and antitumor activity of natural compound aloe emodin derivatives.
abstract: In this study, we have synthesized novel water soluble derivatives of natural compound aloe emodin 4(a-j) by coupling with various amino acid esters and substituted aromatic amines, in an attempt to improve the anticancer activity and to explore the structure-activity relationships. The structures of the compounds were determined by (1) H NMR and mass spectroscopy. Cell growth inhibition assays revealed that the aloe emodin derivatives 4d, 4f, and 4i effectively decreased the growth of HepG2 (human liver cancer cells) and NCI-H460 (human lung cancer cells) and some of the derivatives exhibited comparable antitumor activity against HeLa (Human epithelial carcinoma cells) and PC3 (prostate cancer cells) cell lines compared to that of the parent aloe emodin at low micromolar concentrations.
authors.affiliation: World Class Institute (WCI), Incurable Diseases Research Center, Korea Research Institute of Bioscience and Biotechnology (KRIBB), Ochang, Cheongwon, 363-883, Korea; Department of Chemistry, Govt.S K S J T Institute, Bangalore, Karnataka, 560001, India.
authors.forename: Naraganahalli R
authors.initials: NR
authors.lastname: Thimmegowda
authors.forename: Chanmi
authors.initials: C
authors.lastname: Park
authors.forename: Bettaswamigowda
authors.initials: B
authors.lastname: Shwetha
authors.forename: Krisada
authors.initials: K
authors.lastname: Sakchaisri
authors.forename: Kangdong
authors.initials: K
authors.lastname: Liu
authors.forename: Joonsung
authors.initials: J
authors.lastname: Hwang
authors.forename: Sangku
authors.initials: S
authors.lastname: Lee
authors.forename: Sook J
authors.initials: SJ
authors.lastname: Jeong
authors.forename: Nak K
authors.initials: NK
authors.lastname: Soung
authors.forename: Jae H
authors.initials: JH
authors.lastname: Jang
authors.forename: In-Ja
authors.initials: IJ
authors.lastname: Ryoo
authors.forename: Jong S
authors.initials: JS
authors.lastname: Ahn
authors.forename: Raymond L
authors.initials: RL
authors.lastname: Erikson
authors.forename: Bo Y
authors.initials: BY
authors.lastname: Kim
mesh_terms: D000880:Anthraquinones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D006367:HeLa Cells; D056945:Hep G2 Cells; D006801:Humans; D013329:Structure-Activity Relationship
chemical_list: D000880:Anthraquinones; D000970:Antineoplastic Agents; C518327:aloe emodin
keywords: Hep G2 cells; NCI-H460 cells; aloe emodin; aloe emodin derivatives; antitumor activity; structure activity relationship