Institute for Molecular Bioscience , The University of Queensland , St Lucia , QLD 4072 , Australia.
School of Chemistry and Molecular Bioscience , The University of Queensland , St Lucia , QLD 4072 , Australia.
Org Lett. 2019 Oct 4;21(19):8097-8100. doi: 10.1021/acs.orglett.9b03094. Epub 2019 Sep 23.
Chemical analysis of sp. CMB-F214, yielded five new piperazines, chrysosporazines A-E (-), with structures assigned by spectroscopic and X-ray analyses and biosynthetic considerations. The chrysosporazines - exist as an equilibrium of major and minor -acyl rotamers, while - incorporate an unprecedented hexahydro-6-pyrazino[1,2-]isoquinolin-6-one scaffold. The noncytotoxic chrysosporazines reverse doxorubicin drug resistance in P-glycoprotein overexpressing colon carcinoma cells (SW620 Ad300), with delivering a comparable gain in sensitivity to the positive control, verapamil.
对 sp. CMB-F214 的化学分析得到了五个新的哌嗪化合物，chrysosporazines A-E（-），其结构通过光谱和 X 射线分析以及生物合成考虑来确定。chrysosporazines - 存在主要和次要酰基旋转异构体的平衡，而 - 则包含一个前所未有的六氢-6-吡嗪并[1,2-]异喹啉-6-酮支架。非细胞毒性的 chrysosporazines 逆转了 P-糖蛋白过度表达的结肠癌细胞（SW620 Ad300）中的阿霉素耐药性，其中 与阳性对照维拉帕米相比，对敏感性的提高具有可比性。
