Synthesis and anticancer evaluation of spermatinamine analogues

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:26

Article

Moosa, Basem A.^1,2  Sagar, Sunil³  Li, Song²  Esau, Luke³  Kaur, Mandeep^3,4  Khashab, Niveen M.² 

[1] King Abdullah Univ Sci & Technol, Controlled Release & Delivery CRD Lab, Chem Life Sci & Engn, Thuwal 239556900, Saudi Arabia

[2] King Abdullah Univ Sci & Technol, Ctr Adv Membranes & Porous Mat, Thuwal 239556900, Saudi Arabia

[3] King Abdullah Univ Sci & Technol, Biomol Lab, Computat Biosci Res Ctr, Thuwal 239556900, Saudi Arabia

[4] Univ Witwatersrand, Sch Mol & Cell Biol, Private Bag 3, ZA-2050 Johannesburg, South Africa

关键词: Natural products;    Bromotyrosine;    Spermatinamine;    Cancer;    Cytotoxicity;   

DOI  :  10.1016/j.bmcl.2016.01.083

来源: Elsevier

【 摘 要 】

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 mu M. The obtained results suggested that longer polyamine linker along with aromatic oxime substitution provided the most potent analogue compounds against cancer cell lines. (C) 2016 Elsevier Ltd. All rights reserved.

【 授权许可】

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