Synthesis and anticancer evaluation of spermatinamine analogues

Basem Moosa, Sunil Sagar, Song Li, Luke Esau, Mandeep Kaur, Niveen M. Khashab

Research output: Contribution to journalArticlepeer-review

3 Scopus citations

Abstract

Spermatinamine was isolated from an Australian marine sponge, Pseudoceratina sp. as an inhibitor of isoprenylcystiene carboxyl methyltransferase (Icmt), an attractive and novel anticancer target. Herein, we report the synthesis of spermatinamine analogues and their cytotoxic evaluation against three human cancer cell lines i.e. cervix adenocarcinoma (HeLa), breast adenocarcinoma (MCF-7), and prostate carcinoma (DU145). Analogues 12, 14 and 15 were found to be the most potent against one or more cell lines with the IC50 values in the range of 5 - 10 μM. The obtained results suggested that longer polyamine linker along with aromatic oxime substitution provided the most potent analogue compounds against cancer cell lines.
Original languageEnglish (US)
Pages (from-to)1629-1632
Number of pages4
JournalBioorganic & Medicinal Chemistry Letters
Volume26
Issue number6
DOIs
StatePublished - Feb 4 2016

ASJC Scopus subject areas

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

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