Isolation and structure of homotemsirolimuses A, B, and C.
Article Details
- CitationCopy to clipboard
Kong F, Zhu T, Yu K, Pagano TG, Desai P, Radebaugh G, Fawzi M
Isolation and structure of homotemsirolimuses A, B, and C.
J Nat Prod. 2011 Apr 25;74(4):547-53. doi: 10.1021/np1003388. Epub 2011 Mar 25.
- PubMed ID
- 21438579 [ View in PubMed]
- Abstract
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).
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Temsirolimus Serine/threonine-protein kinase mTOR IC 50 (nM) 1760 N/A N/A Details