Elsevier

Tetrahedron Letters

Volume 59, Issue 33, 15 August 2018, Pages 3206-3209
Tetrahedron Letters

Total synthesis and biological evaluation of nannocystin analogues modified at the polyketide phenyl moiety

https://doi.org/10.1016/j.tetlet.2018.07.028Get rights and content

Highlights

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    10 nannocystin analogues varying at the polyketide phenyl moiety were synthesized.

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    These compounds were tested against both cancer cell lines and normal cell lines.

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    All potent compounds inhibited the growth of both cancerous and normal cell lines.

Abstract

Total synthesis of a focused set of 10 nannocystin analogues 3a–3j modified at the polyketide phenyl moiety was reported. These compounds were evaluated against three cancer cell lines. Compared with the naturally occurring congener 3a, the other synthetic variants either preserved or lose antiproliferative activity at varying degrees. Moreover, the potent analogues also displayed comparable levels of cytotoxicity toward two normal cell lines.

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Acknowledgements

This work was supported by the National Natural Science Foundation of China (Grant No. 81573282) and the National Science Fund for Distinguished Young Scholars (Grant No. 81625021) to Y. Chen, and the National Natural Science Foundation of China (Grant No. 21772101) and the Natural Science Foundation of Tianjin City (Grant No. 17JCYBJC28400) to W. Zhang.

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