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海洋螺旋四烯酮:激发药物研发灵感的生物合成建筑。

Marine Spirotetronates: Biosynthetic Edifices That Inspire Drug Discovery.

机构信息

Department of Chemistry & Biochemistry, University of California San Diego, La Jolla, CA 92093-0358, USA.

出版信息

Mar Drugs. 2019 Apr 19;17(4):232. doi: 10.3390/md17040232.

Abstract

Spirotetronates are actinomyces-derived polyketides that possess complex structures and exhibit potent and unexplored bioactivities. Due to their anticancer and antimicrobial properties, they have potential as drug hits and deserve further study. In particular, abyssomicin C and tetrocarcin A have shown significant promise against antibiotic-resistant and tuberculosis, as well as for the treatment of various lymphomas and solid tumors. Improved synthetic routes to these compounds, particularly the class II spirotetronates, are needed to access sufficient quantities for structure optimization and clinical applications.

摘要

螺旋四烯酮类化合物是放线菌来源的聚酮化合物,具有复杂的结构,并表现出强大而尚未开发的生物活性。由于其抗癌和抗菌特性,它们有可能成为药物靶点,值得进一步研究。特别是深渊霉素 C 和四氢卡奇霉素 A 对对抗生素耐药和结核病具有显著的治疗作用,并且对治疗各种淋巴瘤和实体瘤也有一定的效果。需要改进这些化合物的合成途径,特别是 II 类螺旋四烯酮类化合物,以获得足够数量的化合物进行结构优化和临床应用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4714/6521127/09b1312a8c73/marinedrugs-17-00232-g001.jpg

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