Synthesis of somatostatin analogues containing C-terminal adamantane and their antiproliferative properties

Anna Miyazaki, Yuko Tsuda, Shoji Fukushima, Toshio Yokoi, Tibor Vántus, Gyöngyi Bökönyi, Edit Szabó, Anikó Horváth, György Kéri, Yoshio Okada

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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.

Original languageEnglish
Pages (from-to)5121-5124
Number of pages4
JournalJournal of Medicinal Chemistry
Volume51
Issue number16
DOIs
Publication statusPublished - Aug 28 2008

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ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

Cite this

Miyazaki, A., Tsuda, Y., Fukushima, S., Yokoi, T., Vántus, T., Bökönyi, G., Szabó, E., Horváth, A., Kéri, G., & Okada, Y. (2008). Synthesis of somatostatin analogues containing C-terminal adamantane and their antiproliferative properties. Journal of Medicinal Chemistry, 51(16), 5121-5124. https://doi.org/10.1021/jm701599w