title: Cytotoxic activities of amino acid-conjugate derivatives of abietane-type diterpenoids against human cancer cell lines.
abstract: Nine amino acid conjugate derivatives, each 2-10 and 12-20, were prepared from abietic acid (1) and dehydroabietic acid (11), respectively, and they were evaluated for their cytotoxicities against four human cancer cell lines, i.e., leukemia (HL60), lung (A549), stomach (AZ521), and breast (SK-BR-3). All compounds showed cytotoxicities against HL60 with IC50 values in the range of 2.3-37.3 μM. In addition, most of the derivatives exhibited moderate cytotoxicities against the other cancer cell lines. Among the derivatives, methyl N-[18-oxoabieta-8,11,13-trien-18-yl]-L-tyrosinate (19) exhibited potent cytotoxic activities against four cancer cell lines with IC50 values of 2.3 (HL60), 7.1 (A549), 3.9 (AZ521), and 8.1 μM (SK-BR-3). Furthermore, all derivatives were shown to possess high selective cytotoxic activities for leukemia cells, since they exhibited only weak cytotoxicities against normal lymphocyte cell line RPMI1788.
authors.affiliation: College of Science and Technology, Nihon University, 1-8-14 Kanda Surugadai, Chiyoda-ku, Tokyo 101-8308, Japan. ukiya.motohiko@nihon-u.ac.jp
authors.forename: Motohiko
authors.initials: M
authors.lastname: Ukiya
authors.forename: Takuma
authors.initials: T
authors.lastname: Kawaguchi
authors.forename: Kenta
authors.initials: K
authors.lastname: Ishii
authors.forename: Eri
authors.initials: E
authors.lastname: Ogihara
authors.forename: Yosuke
authors.initials: Y
authors.lastname: Tachi
authors.forename: Masahiro
authors.initials: M
authors.lastname: Kurita
authors.forename: Yoichiro
authors.initials: Y
authors.lastname: Ezaki
authors.forename: Makoto
authors.initials: M
authors.lastname: Fukatsu
authors.forename: Yasunori
authors.initials: Y
authors.lastname: Kushi
authors.forename: Toshihiro
authors.initials: T
authors.lastname: Akihisa
mesh_terms: D045784:Abietanes / Q000737:chemistry* / Q000633:toxicity*; D000596:Amino Acids / Q000737:chemistry*; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D018922:HL-60 Cells; D006801:Humans
chemical_list: D045784:Abietanes; D000596:Amino Acids; D000970:Antineoplastic Agents
keywords: Abietic acid; Amino acids; Cytotoxic activity; Dehydroabietic acid