Leitheiser C J, Rishel M J, Wu X, Hecht S M
Departments of Chemistry and Biology, University of Virginia, Charlottesville, Virginia 22901, USA.
Org Lett. 2000 Oct 19;2(21):3397-9. doi: 10.1021/ol0002469.
The solid-phase syntheses of two deglycobleomycin A(5) analogues were achieved using a commercially available polystyrene resin containing triphenylmethyl-linked spermidine. The final products were deblocked and released from the resin, analyzed, and purified by C(18) reversed phase HPLC and characterized by high-field (1)H NMR spectroscopy and mass spectrometry. The purified products relaxed supercoiled plasmid DNA in a concentration-dependent fashion and to the same extent as authentic material derived from natural BLM A(5).
使用含有三苯甲基连接的亚精胺的市售聚苯乙烯树脂实现了两种去糖博来霉素A(5)类似物的固相合成。最终产物从树脂上脱保护并释放出来，进行分析，通过C(18)反相高效液相色谱法纯化，并通过高场(1)H核磁共振光谱和质谱进行表征。纯化后的产物以浓度依赖的方式使超螺旋质粒DNA松弛，且程度与天然博来霉素A(5)的正品材料相同。
