Mbaba Mziyanda, Mabhula Amanda N, Boel Natasha, Edkins Adrienne L, Isaacs Michelle, Hoppe Heinrich C, Khanye Setshaba D
Department of Chemistry, Rhodes University, Grahamstown 6140, South Africa.
Department of Biochemistry and Microbiology, Rhodes University, Grahamstown 6140, South Africa; Biomedical Biotechnology Research Unit (BioBRU), Rhodes University, Grahamstown 6140, South Africa.
J Inorg Biochem. 2017 Jul;172:88-93. doi: 10.1016/j.jinorgbio.2017.04.014. Epub 2017 Apr 13.
A focused series of novobiocin derivatives containing a ferrocene unit together with their corresponding organic novobiocin analogues have been synthesized in modest to good yields. These compounds were screened for biological activity against a chloroquine-sensitive strain of Plasmodium falciparum (3D7) and human breast cancer cell line (HCC38). With the exception of compounds 5c and 5d, the general trend observed is that incorporation of the ferrocene moiety into novobiocin scaffold resulted in compounds 6a-d/6f showing enhanced activity compared to organic analogues 5a-b and 5e-f.
一系列含有二茂铁单元的新生霉素衍生物及其相应的有机新生霉素类似物已以中等至良好的产率合成。这些化合物针对恶性疟原虫氯喹敏感株（3D7）和人乳腺癌细胞系（HCC38）进行了生物活性筛选。除化合物5c和5d外，观察到的总体趋势是，将二茂铁部分引入新生霉素支架后，与有机类似物5a-b和5e-f相比，化合物6a-d/6f显示出增强的活性。
