2. Academic Validation
  3. Synthesis and anticancer evaluation of spermatinamine analogues

Synthesis and anticancer evaluation of spermatinamine analogues

  • Bioorg Med Chem Lett. 2016 Mar 15;26(6):1629-1632. doi: 10.1016/j.bmcl.2016.01.083.
Basem A Moosa 1,  Sunil Sagar 2,  Song Li 3,  Luke Esau 2,  Mandeep Kaur 4,  Niveen M Khashab 3
Affiliations

Affiliations

  • 1 Controlled Release and Delivery (CRD) Lab, Chemical Life Sciences and Engineering, King Abdullah University of Science and Technology, Thuwal 23955-6900, Saudi Arabia; Center for Advanced Membranes and Porous Materials, King Abdullah University of Science and Technology, Thuwal 23955-6900, Saudi Arabia. Electronic address: [email protected].
  • 2 Biomolecular Lab, Computational Bioscience Research Center, King Abdullah University of Science and Technology, Thuwal 23955-6900, Saudi Arabia.
  • 3 Controlled Release and Delivery (CRD) Lab, Chemical Life Sciences and Engineering, King Abdullah University of Science and Technology, Thuwal 23955-6900, Saudi Arabia; Center for Advanced Membranes and Porous Materials, King Abdullah University of Science and Technology, Thuwal 23955-6900, Saudi Arabia.
  • 4 Biomolecular Lab, Computational Bioscience Research Center, King Abdullah University of Science and Technology, Thuwal 23955-6900, Saudi Arabia; School of Molecular and Cell Biology, University of the Witwatersrand, Private Bag 3, Wits, 2050, Johannesburg, South Africa.
PMID: 26874403 DOI: 10.1016/j.bmcl.2016.01.083
Abstract

Spermatinamine was isolated from an Australian marine Sponge, Pseudoceratina sp. as an inhibitor of isoprenylcysteine 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, that is, 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.

Keywords

Bromotyrosine; Cancer; Cytotoxicity; Natural products; Spermatinamine.

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