| 摘要 |
The present invention relates to imidazole, oxazole and thiazole derivatives of tumor-targeted drug combretastatin A4, and phosphate esters, sulfonate esters or pharmaceutically acceptable salts, glycoside derivatives, solvates thereof, wherein the A-ring comprises a 3,5-dimethoxyphenyl group having a substituent at the 4-position. The pharmacological activity assays have demonstrated that the compounds of the present invention have good in vitro anti-tumor activity and excellent tubulin inhibitory effect. |
| 主权项 |
1. A compound of formula I,or a phosphate ester, a sulfonate ester, a pharmaceutically acceptable salt, a glycoside derivative or a solvate thereof, wherein
A is N, O or S; when A is O or S, R1 is absent; when A is N, R1 is H, CH3, C4H9, R2 is H, CF3, OCF3, OCHF2 or —NHCH3; and R3 is selected from the group consisting of:with the proviso that the following compounds are excluded:
1) when A is N: R1 is CH3, R2 is H, and R3 is 4-N(CH3)2C6H4, 3-F-4-(OCH3)C6H3, 3-(NH2)-4-(OCH3)C6H3 or 3,5-(OCH3)2-4-Br—C6H2; R1 is C4H9, C6H5 or 4-methoxyphenyl, R2 is H, and R3 is 4-N(CH3)2C6H4; and 2) when A is O: R2 is H, and R3 is 3,5-(OCH3)2-4-Br—C6H2. |
