Isolation and Structure of Homotemsirolimuses A, B, and C

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• 作者：Fangming Kong ; Tianmin Zhu ; Ker Yu ; Thomas G. Pagano ; Parimal Desai ; Galen Radebaugh ; Mahdi Fawzi
• 刊名：Journal of Natural Products
• 出版年：2011
• 出版时间：April 25, 2011
• 年：2011
• 卷：74
• 期：4
• 页码：547-553
• 全文大小：824K
• 年卷期：v.74,no.4(April 25, 2011)
• ISSN：1520-6025

文摘

Homotemsirolimuses A, B, and C (2a, 2b, 2c) were found to be minor components of a temsirolimus preparation made from rapamycin. These three temsirolimus analogues are derived from the corresponding rapamycin analogues, homorapamycins A, B, and C (1a, 1b, 1c) produced by the strain Streptomyces hygroscopicus. The structures of homotemsirolimuses A, B, and C were determined by spectroscopic methods. These compounds were tested for mTOR kinase inhibition and in two proliferation assays using LNCap prostate and MDA468 breast cancer cells. The results suggested that the mTOR inhibition and antiproliferation potencies for 2a, 2b, and 2c are comparable to those of rapamycin (1) and temsirolimus (2).