4.8 Article

Englerin A, a Selective Inhibitor of Renal Cancer Cell Growth, from Phyllanthus engleri

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ORGANIC LETTERS
卷 11, 期 1, 页码 57-60

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AMER CHEMICAL SOC
DOI: 10.1021/ol802339w

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  1. NIH
  2. National Cancer Institute
  3. Center for Cancer Research
  4. Developmental Therapeutics Program in the Division of Cancer Treatment
  5. Diagnosis of the National Cancer Institute
  6. NATIONAL CANCER INSTITUTE [ZICBC010469] Funding Source: NIH RePORTER

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An extract from Phyllanthus engleri was identified in a bioinformatic analysis of NCI 60-cell natural product extract screening data that selectively Inhibited the growth of renal cancer cell lines. Bioassay-guided fractionation yielded two new gualane sesquiterpenes, englerins A (1) and B (2). Englerin A showed 1000-fold selectivity against six of eight renal cancer cell lines with GI(50) values ranging from 1-87 nM. The structures of I and 2 and their relative stereochemistry were established by spectroscopic methods,

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