Zhou Rong, Liao Xiaojian, Li Hangbin, Li Jing, Feng Pengju, Zhao BingXin, Xu Shihai
Department of Chemistry, Jinan University, Guangzhou, China.
Front Chem. 2018 Jun 13;6:212. doi: 10.3389/fchem.2018.00212. eCollection 2018.
A novel indole alkaloid, misszrtine A (), was isolated from marine sponge-derived fungus sp. SCSIO XWS03F03. The planar structure of was assigned by analysis of spectroscopic data, the absolute configuration of which was unambiguously determined by total synthesis. Compound represents the first example of -isopentenyl tryptophan methyl ester with a phenylpropanoic amide arm, which exhibited a potent antagonistic activity on HL60 (IC = 3.1 μM) and LNCaP (IC = 4.9 μM) cell lines. Bioactivity evaluation reveals that functional group on indole nitrogen of has a great effect on its cytotoxity, which provides a mean to probe the structure-activity relationships of .
从海洋海绵来源的真菌短密青霉SCSIO XWS03F03中分离得到一种新型吲哚生物碱——米氏菌素A()。通过光谱数据分析确定了其平面结构,并通过全合成明确确定了其绝对构型。化合物代表了具有苯丙酰胺臂的β-异戊烯基色氨酸甲酯的首个实例,该化合物对HL60(IC = 3.1 μM)和LNCaP(IC = 4.9 μM)细胞系表现出强效拮抗活性。生物活性评估表明,米氏菌素A吲哚氮上的官能团对其细胞毒性有很大影响,这为探究米氏菌素A的构效关系提供了一种手段。