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    Concise total synthesis of diketopiperazine PJ147, obtained from mycelium of Gliocladium sp. YUP08, has been achieved in seven steps with 43.5% overall yield. Biological evaluation of PJ147 exhibited strong inhibiting activity against A375-S2, Hela, P388, A-549, HL-60, and BEL-7420 cell lines. Thus, eight derivatives of PJ147 with high water solubility were also synthesized to facilitate the in vivo bioassay of this kind of diketopiperazines.


    Xue-Zheng Li, Gang Chen, Hai-Feng Wang, Hui-Ming Hua, Yue-Hu Pei. Synthesis and bioactivity of diketopiperazine PJ147 and its derivatives from Gliocladium sp. YUP08. Journal of Asian natural products research. 2014;16(7):764-9

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    PMID: 24827395

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