2-(2-phenylethenyl) 1,3-benzodiazepine derivatives useful for the treatment of cancer

摘要

The present invention provides compounds of formula (1) acting as protein kinase (PK) and receptor kinase (RK) signaling modulators. The invention further provides methods of their preparation, pharmaceutical compositions including such compounds, and methods of using these compounds and compositions, especially as anti-cancer agents for preventions and treatments of PK- and RK-related disorders, in particular cancer. (I) wherein A is H or CN; Z is S, SO or S02; X1, X2, X3, X4, X5, Y1 and Y2 are each independently selected from H, halogen, alkyl, haloalkyl and OR1; and Y3 and Y4 are each OR1, wherein each R1 is independently H, C1-C4 alkyl, acyl, —(CH2CH20)n wherein n is an integer of 1 to 20, or a functional group that gives rise to hydroxyl upon hydrolysis.;

主权项

1. A compound represented by the structure of formula 1: wherein A is H or CN; Z is S, SO or SO2; X1, X2, X3, X4, X5, Y1 and Y2 are each independently selected from H, halogen, alkyl, haloalkyl and OR1; and Y3 and Y4 are each OR1, wherein each R1 is independently H, C1-C4 alkyl, acyl, —(CH2CH2O)n wherein n is an integer of 1 to 20, or a functional group that gives rise to hydroxyl upon hydrolysis, including salts, hydrates, solvates, polymorphs, optical isomers, geometrical isomers, enantiomers, diastereomers, and mixtures thereof.