ACENAFTO-HETEROCYCLIC COMPOUNDS, THEIR INCLUSION CONNECTIONS AND COMPLEXES WITH CYCLODEXTRIN, AND THEIR APPLICATIONS FOR OBTAINING ANALOGUES OF THE PROTEIN Dietary supplement, protein inhibitors of the BCL-2 family

摘要

1. An acenaphtho-heterocyclic compound having the following structural formula: where: (I) R = XR, thiophenomethoxyl, thiophenomethylamino or thiomorpholinyl, R = H, R = H, R = CN, COOH, COOR or CONHR; (II) R = H, R = XR, thiophenomethoxyl, thiophenomethylamino or thiomorpholinyl, R = H, R = CN, COOH, COOR or CONHR; (III) R = H, R = H, R = H, XR, tetrahydropyran-4-hydroxy-, tetrahydrothiopyran -4-hydroxy-, thiophenomethoxyl, thiophenomethylamino or thiomorpholinyl, R = CN; (IV) R = XR, R = H, R = XR, R = CN; where: X = O, S, carbonyl, ester or amide; R = a: (CH) Ar- (ortho, meta, pair) Y, Y = CH, NO, Ph, F, Cl, Br, CF, OCH, SCH or NH; n = 0-4; b: tetrahydropyran or tetrahydrothiapiran; R = CH or CH; R = CH, CH or Ar. 2. The cyclodextrin inclusion compound and the acenaphtho-heterocyclic compound according to claim 1, characterized in that the cyclodextrin inclusion compound is prepared as follows: (1) the amount of cyclodextrin is weighed and added to water, then heated with stirring until a saturated solution is formed, where cyclodextrin is β-cyclodextrin, γ-cyclodextrin, 2-hydroxypropyl-β-cyclodextrin, methyl-β-cyclodextrin or hydroxypropyl-γ-cyclodextrin; (2) the amount of acenaphtho-heterocyclic compound is weighed for inclusion, where the molar ratio between compound and cyclodextrin is 1: 3-10; (3) the acenaphtho-heterocyclic compound is dissolved for inclusion in acetone at a concentration of 5-10 mg / ml, and the resulting solution is added dropwise to an aqueous solution cyclodextrin alternately, then heated and stirred for 1-6 days at a temperature of 40-65 ° C until the precipitate is separated; (4) filter the above solution and wash the filtered precipitate with a little distilled water, then wash the compounds