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Asymmetric Synthesis and Biological Activities of Pactamycin-Inspired Aminocyclopentitols
Organic Letters ( IF 5.2 ) Pub Date : 2018-01-10 00:00:00 , DOI: 10.1021/acs.orglett.7b03681
Corey J. Brumsted 1 , Evan L. Carpenter , Arup K. Indra , Taifo Mahmud 1
Affiliation  

Pactamycin is a structurally unique aminocyclitol antibiotic with broad-spectrum cell growth inhibitory activity. To explore the bountiful activity of the aminocyclitol core of pactamycin, an efficient, modular, and asymmetric synthesis of aminocyclopentitols resembling the pactamycin pharmacophore has been developed employing a SmI2-mediated imino-pinacol coupling strategy. Two of the compounds exhibited antitumor activity against A375 melanoma cells.

中文翻译:

受到霉素启发的氨基环戊糖醇的不对称合成及其生物活性

泛霉素是一种结构独特的氨基环醇抗生素,具有广谱细胞生长抑制活性。为了探索pactamycin氨基环醇核心的丰富活性,已开发出一种有效的,模块化的,不对称的类似于pactamycin药效团的氨基环戊醇合成方法,采用了SmI 2介导的亚氨基-频哪醇偶联策略。其中两种化合物对A375黑色素瘤细胞具有抗肿瘤活性。
更新日期:2018-01-10
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