Synthesis and bioactivity of a Goralatide analog with antileukemic activity

Zhiliang Li, Iryna Oleksandrivna Lebedyeva, Vita M. Golubovskaya, William G. Cance, Khalid A. Alamry, Hassan M. Faidallah, C. Dennis Hall, Alan R. Katritzky

Research output: Contribution to journalArticle

Abstract

Natural tetrapeptide Goralatide (AcSDKP) is a selective inhibitor of primitive haematopoietic cell proliferation. It is not stable in vivo and decomposes within 4.5 min when applied to live cells. In this work we developed an analog of Goralatide that exhibits cytotoxicity towards human myeloid HL-60, HEL, Nalm-6 leukemia cells, endothelial HUVEC, glioblastoma U251 and transformed kidney 293T cells. The Goralatide analog showed significant stability in organic solution with no tendency to degrade oxidatively.

Original languageEnglish (US)
Pages (from-to)5056-5060
Number of pages5
JournalBioorganic and Medicinal Chemistry
Volume23
Issue number15
DOIs
Publication statusPublished - Jul 23 2015

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Keywords

  • Anticancer
  • Antileukemic
  • Goralatide
  • Peptide
  • Peptidomimetic

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

Cite this

Li, Z., Lebedyeva, I. O., Golubovskaya, V. M., Cance, W. G., Alamry, K. A., Faidallah, H. M., ... Katritzky, A. R. (2015). Synthesis and bioactivity of a Goralatide analog with antileukemic activity. Bioorganic and Medicinal Chemistry, 23(15), 5056-5060. https://doi.org/10.1016/j.bmc.2015.04.061