| 摘要 |
The present invention belongs to the field of natural medicine and pharmaceutical chemistry, and specifically relates to novel 2-aminated methylene or 2-esterified methylene tanshinone I derivatives of formula (I) or a pharmaceutically acceptable salt thereof, to a process for the preparation of these compounds, compositions containing such compounds and their use in preparing antineoplastic medicaments. When X is nitrogen, formula I indicates 2-aminated methylene tanshinone I; when X is oxygen, formula I indicates 2-esterified methylene tanshinone I.; |
| 主权项 |
1. A 2-aminated methylene or 2-esterified methylene tanshinone I derivative of formula (I), or a pharmaceutically acceptable salt thereof, X is nitrogen or oxygen; when X is nitrogen, Y is (R1R2), then the compound of formula (I) is 2-aminated methylene tanshinone I of formula I-1; and when X is oxygen, Y is —(CO)R, then the compound of formula (I) is 2-esterified methylene tanshinone I of formula I-2, wherein R is selected from the group consisting of H, substituted or unsubstituted C2-C18 alkyl, substituted or unsubstituted C2-C18 alkenyl or alkynyl, substituted or unsubstituted C3-C7 cycloalkyl or cycloalkenyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl or heterocyclyl; R1 is H, methyl or ethyl; R2 is C1-C3 alkyl substituted with a substituent selected from the group consisting of hydroxyl, C1-C6 alkylcarbonyloxy, cycloalkylcarbonyloxy, heterocyclyl carbonyloxy, amino-acid ester group wherein the amino is optionally substituted with C1-C6 alkoxycarbonyl, and C2-C8 dicarboxylic ester group optionally containing carbon-carbon double bond wherein one carboxyl is optionally esterified with C1-C6 alkyl; and each of the aforementioned substituted group is optionally substituted by one or more substituents selected from the group consisting of halogen, nitro, cyano, amino, hydroxyl, thiol, carboxyl, C1-C6 substituted amino, C1-C6 alkoxy, and C1-C6 alkylthio. |
