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US 2016/0355493 A1Published application
Caffeic acid derivatives for anti-angiogenesis
AssigneesTaipei Medical University, China Medical University
InventorsChieh-Hsi Wu, Yueh-Hsiung Kuo, Chun-Hsu Pan
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Abstract
The present invention develops a series of methyl caffeate derivatives having biological activity in anti-angiogenesis. The present invention suggests that the compounds of the invention possess inhibiting angiogenesis through regulation of VEGF/VEGFR-2 and its downstream signaling cascades in the vascular endothelial cells (VECs).
Claims17
A compound having the following formula (I) or (II),
- wherein
- X is O, N, or S;
- R1 is C1-10alkyl, C2-10alkenyl or C2-10alkynyl, unsubstituted or substituted by halogen, NH2, NO2, CN, OH, —CHO, C(O)2C1-10alkyl, C(O)2C1-10alkenyl or C(O)2C1-10alkynyl;
- R2 is C1-10alkoxy, C2-10alkenyloxy, C2-10alkynyloxy, —O-acetyl, hydroxy, formyl, halide, CN, NO2, SH, NH2, amido, sulfonyl, or sulfonamido;
- R3 is C1-10alkyl, C2-10alkenyl, C2-10alkynyl, C(O)2C1-10alkyl, C(O)2C1-10alkenyl or C(O)2C1-10alkynyl;
- R4 is C1-10alkoxy, C2-10alkenyloxy, C2-10alkynyloxy, —O-acetyl, hydroxy, formyl, halide, CN, NO2, SH, NH2, amido, sulfonyl, or sulfonamido;
- R5 is OH, C1-10alkoxy, C2-10alkenyloxy, C2-10alkynyloxy, —O-acetyl, hydroxy, formyl, halide, CN, NO2, SH, NH2, amido, sulfonyl, or sulfonamido;
- and
- R6 is H, halogen, OH, NH2, CN or NO2;
- or a stereoisomer thereof, or an enantiomer thereof, or a prodrug thereof or a pharmaceutically acceptable salt thereof.
7 more elements
Dependencies are inferred from the claim text.