Production and use for taxol and muramic acyl dipeptide conjugate substance of immune reinforcer
Patent Information
- Authority / Receiving Office
- CN · China
- Current Assignee / Owner
- INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
- Publication Date
- 2005-12-28
- Estimated Expiration
- Not applicable · inactive patent
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Abstract
Description
technical field
[0001] The invention relates to a conjugate of anticancer prodrug paclitaxel and muramyl dipeptide (muramyl alanyl isoglutamine) and a preparation method thereof. Specifically, three series of compounds conjugated with muramyl dipeptide at the 7-O position, 2'-O position and 3'-N position of paclitaxel and their preparations. Compared with paclitaxel, the conjugate involved in the invention has better water solubility and good biological activity. Background technique
[0002] Paclitaxel is one of the natural diterpenoids isolated from the genus Taxus. As early as 1962, the U.S. Department of Agriculture (USDA) collected Pacific yew (Taxus brevifolia) bark for the U.S. National Cancer Institute (NCI) to screen anticancer active ingredients. In 1963, Wall and Wani extracted the crude extract; in 1969, it was determined that the active ingredient in the crude extract was paclitaxel. In 1971, Wani et al isolated pure paclitaxel and determined its structure by...