Synthesis and bioactivity of diketopiperazine PJ147 and its derivatives from Gliocladium sp. YUP08

Xue-Zheng LiDepartment of Pharmacy, Affiliated Hospital of Yanbian University, Yanji133000, China

Gang ChenSchool of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang110016, China;Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University), Ministry of Education, Shenyang110016, ChinaCorrespondence[email protected]

Hai-Feng WangSchool of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang110016, China;Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University), Ministry of Education, Shenyang110016, China

Hui-Ming HuaSchool of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang110016, China;Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University), Ministry of Education, Shenyang110016, China

Yue-Hu PeiSchool of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang110016, China;Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University), Ministry of Education, Shenyang110016, China

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.

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Synthesis and bioactivity of diketopiperazine PJ147 and its derivatives from Gliocladium sp. YUP08

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Synthesis and bioactivity of diketopiperazine PJ147 and its derivatives from Gliocladium sp. YUP08

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