Synthesis and anticancer evaluation of spermatinamine analogues

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.

Citation
Synthesis and anticancer evaluation of spermatinamine analogues 2016 Bioorganic & Medicinal Chemistry Letters

Publisher
Elsevier BV

Journal
Bioorganic & Medicinal Chemistry Letters

DOI
10.1016/j.bmcl.2016.01.083

PubMed ID
26874403

Additional Links
http://linkinghub.elsevier.com/retrieve/pii/S0960894X16300919

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