Literature DB >> 26400369

Total synthesis and absolute stereochemistry of the proteasome inhibitors cystargolides A and B.

Rodolfo Tello-Aburto1, Liam P Hallada, Doleshwar Niroula, Snezna Rogelj.   

Abstract

The absolute stereochemistry of the cystargolides was determined by total synthesis. Evaluation of synthetic cystargolides and derivatives showed that the natural (2S,3R) stereochemistry is essential for activity. Moreover, benzyl esters (-)-10 and (-)-15 were found to be about 100 times more potent, and to selectively kill MCF-7 cancerous cells.

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Year:  2015        PMID: 26400369      PMCID: PMC4629797          DOI: 10.1039/c5ob01821h

Source DB:  PubMed          Journal:  Org Biomol Chem        ISSN: 1477-0520            Impact factor:   3.876


  18 in total

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  5 in total

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