Isolation and structure of homotemsirolimuses A, B, and C.

Article Details

Citation

Copy 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