Muta-mycosynthesis of naphthalene analogs.
Muta-mycosynthesis of naphthalene analogs.
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DOI：
10.1021/acs.orglett.5b00335
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发表时间：
2015-03
期刊：
影响因子：
5.2
通讯作者：
Yuan-ru-hua Tian;Nan Jiang;A. Zhang;Chao-Jun Chen;Xin-Zhao Deng;Wen Jing Zhang;R. Tan
中科院分区：
文献类型：
--
作者：
Yuan-ru-hua Tian;Nan Jiang;A. Zhang;Chao-Jun Chen;Xin-Zhao Deng;Wen Jing Zhang;R. Tan
介绍了一种突变合成策略，通过产生和使用埃氏炭层壳的ΔpksTL突变菌株，用于具有定向取代模式和新框架的基于萘的分子（mutadalesols A-F）的真菌合成。（±）-Mutadalesol A及其（+）-对映体具有细胞毒性，其（-）-对映体抑制Toll样受体5（TLR 5）。真菌寡聚酮中间体与5-氨基萘-1-醇（ANL）的培养反应性被证明，揭示了对药物发现管道中有价值的非天然分子库的生物正交访问。
A mutasynthetic strategy is introduced for the mycosynthesis of naphthalene-based molecules (mutadalesols A-F) with directed substitution patterns and new frameworks by generating and using the ΔpksTL mutant strain of Daldinia eschscholzii. (±)-Mutadalesol A and its (+)-enantiomer are cytotoxic, and its (-)-enantiomer inhibits Toll-like receptor 5 (TLR5). The in-culture reactability of fungal oligoketide intermediates with 5-aminonaphthalen-1-ol (ANL) is demonstrated, shedding light on bioorthogonal accesses to unnatural molecule libraries valuable in drug discovery pipelines.