Center for Marine Biotechnology and Biomedicine, Scripps Institution of Oceanography, University of California at San Diego, La Jolla, CA 92093, USA.
Bioorg Med Chem Lett. 2012 Jan 1;22(1):683-8. doi: 10.1016/j.bmcl.2011.10.054. Epub 2011 Oct 24.
Bioassay-guided fractionation of two cyanobacterial extracts from Papua New Guinea has yielded hoiamide D in both its carboxylic acid and conjugate base forms. Hoiamide D is a polyketide synthase (PKS)/non-ribosomal peptide synthetase (NRPS)-derived natural product that features two consecutive thiazolines and a thiazole, as well as a modified isoleucine residue. Hoiamide D displayed inhibitory activity against p53/MDM2 interaction (EC(50)=4.5 μM), an attractive target for anticancer drug development.
基于生物测定的导向分离，从巴布亚新几内亚的两种蓝藻提取物中得到了霍亚酰胺 D 的羧酸形式和共轭碱形式。霍亚酰胺 D 是一种聚酮合酶（PKS）/非核糖体肽合酶（NRPS）衍生的天然产物，具有两个连续的噻唑啉和一个噻唑，以及一个修饰的异亮氨酸残基。霍亚酰胺 D 对 p53/MDM2 相互作用具有抑制活性（EC50=4.5 μM），是抗癌药物开发的一个有吸引力的靶点。
