[EN] GLUCOSE CONJUGATES OF TRIPTOLIDE, ANALOGS AND USES THEREOF<br/>[FR] CONJUGUÉS GLUCOSE DE TRIPTOLIDE, ANALOGUES ET UTILISATIONS CORRESPONDANTS
申请人:UNIV JOHNS HOPKINS
公开号:WO2017136739A1
公开(公告)日:2017-08-10
Provided are compounds generated by conjugation of triptolide with glucose to form glucose-triptolide conjugates, provides compounds with effective anti -proliferative activity and improved tolerability as compared to naturally occurring triptolide compounds.
TRIPTOLIDE DERIVATIVES AND PREPARATION METHOD AND USE THEREOF
申请人:Hong Kong Baptist University
公开号:US20160362691A1
公开(公告)日:2016-12-15
Tripyolide-nucleic acid aptamer derivatives, a preparation method and use thereof are shown. The structure of the triptolide-nucleic acid aptamer derivatives is as shown by formula I, wherein the definitions of R
1
-R
7
, G, A, B, M, Z and X are described. The present invention uses a nucleic acid aptamer and triptolide or modified compounds thereof as the starting materials, and introduces a linking group A at the C-14 hydroxyl group, epoxy groups and five-membered ring lactones in triptolide, then connects it to a nucleic acid aptamer B, and obtains the triptolide-nucleic acid aptamer derivatives. The triptolide-nucleic acid aptamer derivatives of the present invention have the characteristics of good targeting, a high anti-cancer activity, low toxicity and side effects, good water solubility and high bioavailability, and the preparation method of the present invention is scientific and reasonable and has a controllable quality and good repeatability, and is thereby suitable for production.