Orally bioavailable caffeic acid related anticancer drugs

摘要

The present invention concerns compounds and their use to treat cell proliferative diseases such as cancer. Compounds of the present invention display significant potency as inhibitors of Jak2/STAT3 pathways and downstream targets and inhibit the growth and survival of cancerous cell lines.

主权项

1. A compound selected from the group consisting of: wherein R1 is —H or cyano and R2 is heteroatom-unsubstituted C3-C7-cycloalkyl; wherein X1 is halo and R3 is heteroatom-unsubstituted C3-C7-cycloalkyl, C6-C10-aryl, or C7-C10-aralkyl; wherein X2 is halo and R4 is hydroxy or heteroatom-unsubstituted C1-C10-acyloxy; wherein:
X3 is halo or heteroatom-unsubstituted C1-C10-alkyl or C1-C10-alkoxy,R5 is —H or cyano, andR6 is heteroatom-unsubstituted C3-C7-cycloalkyl, C1-C10-acyloxy, C6-C10-aryl, or C7-C10-aralkyl; wherein:
X4 is halo or heteroatom-unsubstituted C1-C10-alkyl or C1-C10-alkoxy,R7 is —H or cyano, andR8 is a heteroatom-unsubstituted C3-C7-cycloalkyl, C1-C10-acyloxy, C6-C10-aryl, or C7-C10-aralkyl; wherein:
X5 is heteroatom-unsubstituted C1-C10-alkyl or C1-C10-alkoxy,R9 is —H or cyano, andR10 is a heteroatom-unsubstituted C3-C7-cycloalkyl, C1-C10-acyloxy, C6-C10-aryl, or C7-C10-aralkyl; and wherein:
A is —C(O)—, andX6 is halo or heteroatom-unsubstituted C1-C10-alkyl or C1-C10-alkoxy,R11 is heteroatom-unsubstituted C3-C7-cycloalkyl, C1-C10-acyloxy, C6-C10-aryl, or C7-C10-aralkyl; or a pharmaceutically acceptable salt or tautomer thereof.