| 标题 |
Synthetic efforts towards brocazine F & G: Total synthesis and new chemical screening libraries
brocazine F&G的合成努力：全合成和新的化学筛选库
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American Chemical Society ABSTRACT:Brocazines are a family of natural products bearing a disulfide diketopiperazine core that was isolated by Meng et al in 2014 and 2016 from an endophytic fungus derived from the marine mangrove plant Avicennia marina named Penicillium brocae MA-231. Seven different brocazines (A-G) and three different spyrobrocazines were isolated and of those brocazine F showed the strongest activity against prostate cancer cell line DU145 (IC50 of 1.7 μM) and lung cancer cell line NCI-H460 (IC50 of 0.89 μM). Brocazine G showed strong activity against ovarian carcinoma cell line A2780 (IC50 of 0.664 μM), ovarian endometrioid adenocarcinoma A2780 CisR cells (IC50 of 0.661 μM) as well as possessing strong and selective activity against human pathogen Staphylococcus aureus (MIC of 0.25 μg/mL). Given the potent cytotoxicity of brocazine F and G and their intriguing polycyclic core structure, our laboratory devised a total synthesis route to access this family. |
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