title: Synthesis of somatostatin analogues containing C-terminal adamantane and their antiproliferative properties.
abstract: On the basis of the structure of somatostatin analogue TT-232 (1), which exhibited a highly potent antitumor activity, we synthesized small linear peptide derivatives and evaluated their antitumor and apoptotic activity. Of them, Boc-Tyr-D-Trp-1-adamantylamide (5) had the most potent cell antiproliferative activity in SW480 and A431 cell lines, which was supported in A431 cell lines by FACS analysis that demonstrated a major increase in DNA fragmentation in the subG1 fraction.
authors.affiliation: Faculty of Pharmaceutical Sciences, Department of Medicinal Chemistry, Kobe Gakuin University, Nishi-ku, Kobe, 651-2180, Japan.
authors.forename: Anna
authors.initials: A
authors.lastname: Miyazaki
authors.forename: Yuko
authors.initials: Y
authors.lastname: Tsuda
authors.forename: Shoji
authors.initials: S
authors.lastname: Fukushima
authors.forename: Toshio
authors.initials: T
authors.lastname: Yokoi
authors.forename: Tibor
authors.initials: T
authors.lastname: Vántus
authors.forename: Gyöngyi
authors.initials: G
authors.lastname: Bökönyi
authors.forename: Edit
authors.initials: E
authors.lastname: Szabó
authors.forename: Anikó
authors.initials: A
authors.lastname: Horváth
authors.forename: György
authors.initials: G
authors.lastname: Kéri
authors.forename: Yoshio
authors.initials: Y
authors.lastname: Okada
mesh_terms: D000218:Adamantane / Q000737:chemistry*; D000970:Antineoplastic Agents / Q000138:chemical synthesis*; D017209:Apoptosis / Q000187:drug effects*; D049109:Cell Proliferation / Q000187:drug effects; D006801:Humans; D013004:Somatostatin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D014407:Tumor Cells, Cultured / Q000187:drug effects
chemical_list: D000970:Antineoplastic Agents; D013004:Somatostatin; D000218:Adamantane