Total synthesis and biological evaluation of nannocystin analogues modified at the polyketide phenyl moiety |
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| Authors: | Yunfeng Tian Yahui Ding Xiaolong Xu Yanju Bai Yang Tang Xin Hao Weicheng Zhang Yue Chen |
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| Affiliation: | The State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy, and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin 300071, People’s Republic of China |
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| 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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| Keywords: | Nannocystin Structure–activity relationship Anticancer Eukaryotic elongation factor 1A |
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