Abstract
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.
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Acknowledgments
This paper was financially supported by projects of Shenyang science and technology plans F12-156-9-00 and by Program for Innovative Research Team of the Ministry of Education and Program for Liaoning Innovative Research Team in University.