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NOVEL INHIBITORS OF ANTIAPOPTOTIC BCL-2 PROTEIN

机译:抗凋亡BCL-2蛋白的新型抑制剂

摘要

The invention provides a method of synthesis of a compound for inhibiting BCL-2 function. The method includes selecting a concentration of a indolin-2-one dissolved in alcohol. The indolin-2-one dissolved in alcohol is then treated with an aldehyde derivative in the presence of piperidine to obtain a reaction mixture. The reaction mixture is refluxed and then cooled under reduced pressure to obtain a precipitate. The precipitate is subsequently purified to obtain the compound and derivatives thereof. The invention provides a compound for inhibiting BCL-2 function. The invention further provides a pharmaceutical composition including the compound for inhibiting BCL-2 function. A method of a managing at least one condition associated with increased expression of BCL-2. A kit for inducing apoptosis or manging at least one condition associated with over expression of BCL-2 is also provided.
机译:本发明提供了用于抑制BCL-2功能的化合物的合成方法。该方法包括选择溶解在醇中的吲哚-2-酮的浓度。然后在哌啶的存在下用醛衍生物处理溶于醇的吲哚-2-酮,得到反应混合物。将反应混合物回流,然后在减压下冷却以获得沉淀物。随后将沉淀物纯化以获得化合物及其衍生物。本发明提供了一种抑制BCL-2功能的化合物。本发明进一步提供了包含用于抑制BCL-2功能的化合物的药物组合物。一种管理与BCL-2表达增加有关的至少一种状况的方法。还提供了一种试剂盒,其用于诱导凋亡或处理与BCL-2的过表达有关的至少一种状况。

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