Moosa Basem A, Sagar Sunil, Li Song, Esau Luke, Kaur Mandeep, Khashab Niveen M
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.
Biomolecular Lab, Computational Bioscience Research Center, King Abdullah University of Science and Technology, Thuwal 23955-6900, Saudi Arabia.
Bioorg Med Chem Lett. 2016 Mar 15;26(6):1629-1632. doi: 10.1016/j.bmcl.2016.01.083. Epub 2016 Feb 4.
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.
精胺素是从澳大利亚海洋海绵 Pseudoceratina sp. 中分离出来的，它是异戊烯基半胱氨酸羧基甲基转移酶（Icmt）的抑制剂，Icmt 是一个具有吸引力的新型抗癌靶点。在此，我们报道了精胺素类似物的合成及其对三种人类癌细胞系，即宫颈腺癌（HeLa）、乳腺腺癌（MCF-7）和前列腺癌（DU145）的细胞毒性评估。发现类似物 12、14 和 15 对一种或多种细胞系最具活性，IC50 值在 5-10 μM 范围内。所得结果表明，较长的多胺连接基与芳香肟取代相结合可提供针对癌细胞系的最具活性的类似物化合物。
