ACENAPHTHO HETEROCYCLE COMPOUNDS, CYCLODEXTRIN INCLUSION COMPOUNDS AND COMPLEXES, AND USES IN THE MANUFACTURES OF BH3 PROTEIN ANALOGUE, BCL-2 FAMILY PROTEIN INHIBITORS THEREOF

摘要

Acenaphtho heterocycle compounds, cyclodextrin inclusion compounds and complexes, and the uses in the manufactures of BH3 protein analogue, Bcl-2 family protein inhibitors thereof. The acenaphtho heterocycle compounds are obtained by introducing oxy group, thio group, carbonyl group, ester group or acyl group on the 3, 4, 6 position of 8-oxo-8H-acenaphtho[1,2-b]pyrrole-9-carbonitrile respectively, or furthermore substituting 9-cyano with carboxyl group, ester group or amide group. They can simulate BH3-only protein, competitively binding and antagonizing Bcl-2, Bcl-xL and Mcl-1 proteins in vitro or intracellular, to induce cell apoptosis. And the cyclodextrin inclusion compounds and complexes can improve the effects. They all can be used in the manufactures of anticancer compounds.