1-OXO/ACYLATION-14-ACYLATED ORIDONIN DERIVATIVE, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF

摘要

The present invention relates to the fields of natural medicine and medicinal chemistry, and more particularly to a 1-oxo/acylated-14-acylated oridonin derivative of a general formula (I) or a pharmaceutically acceptable salt thereof, a method for preparing the compounds, a pharmaceutical composition comprising the compounds, and application thereof in preparation of antitumor drugs.;

主权项

1. A 1-oxo/acylated-14-acylated oridonin derivative of formula (I), or a pharmaceutically acceptable salt thereof, wherein W is oxo or —O(CO)R′; L is selected from the group consisting of direct bond, —(CH═CH)n—, piperidinocarbonyl, piperidinosulfonyl, cyclohexylaminocarbonyl, and cyclohexylaminosulfonyl; n is 1 or 2; R′ is C1-C6 alkyl; R is aryl, heteroaryl, C3-C7cycloalkyl, C3-C7 cycloalkenyl, heterocyclyl, C1-C6 alkyl, amino C1-C6 alkyl, (C1-C6 alkyl)amino C1-C6 alkyl, di(C1-C6 alkyl)amino C1-C6 alkyl, hydroxyl C1-C6 alkyl, aryl C1-C6 alkyl, or heteroaryl C1-C6 alkyl; wherein, the aryl, heteroaryl, C3-C7cycloalkyl, C3-C7cycloalkenyl and heterocyclyl are respectively optionally substituted with a substituent selected from the group consisting of halogen, amino, C1-C6 alkylamino, di(C1-C6alkyl)amino, nitro, cyano, hydroxyl, C1-C6 alkoxy, C1-C6haloalkoxy, thiol, C1-C6 alkylthio, C1-C6 alkyl, hydroxyl C1-C6 alkyl and C1-C6haloalkyl; the C3-C7cycloalkenyl is also optionally substituted with carboxyl; with a proviso that when W is —O(CO)CH3, L-R is not methyl.