首页> 外国专利> dansyl carbazole compound, method for treating cancer in a subject, method for reducing dna menthyltransferase activity in a cell, method for increasing expression of family domain 1a (rassf1a) association in a cell, cell identification methods Method of determining whether one or more cells of a subject are cancer cells, pharmaceutical composition and kit.

dansyl carbazole compound, method for treating cancer in a subject, method for reducing dna menthyltransferase activity in a cell, method for increasing expression of family domain 1a (rassf1a) association in a cell, cell identification methods Method of determining whether one or more cells of a subject are cancer cells, pharmaceutical composition and kit.

机译:丹磺酰基咔唑化合物,治疗受试者癌症的方法,降低细胞中dna薄荷基转移酶活性的方法,增加细胞中家族结构域1a(rassf1a)关联的表达的方法,细胞鉴定方法确定一种或多种细胞的方法受试者是癌细胞,药物组合物和试剂盒。

摘要

The invention provides carbazole compounds, and prodrugs therefor, comprising a heterogroup coupled to an aryl group, wherein the heterogroup is selected from the group consisting of SO 2 , S=O, C=O, NH, and PO 3 . The aryl group may be substituted with one or more substituents selected from the group consisting of OH, NH 2 , NR 1 R 2 , NHR 1 , OCH 3 , OCHR 1 R 2 , OCH 2 R 1 , OCR 1 R 2 R 3 , C=O, or S=O, wherein R 1 , R 2 , and R 3 are alkyl groups, optionally wherein the heterogroup coupled to the aryl group is a dansyl group, and optionally wherein the heterogroup coupled to the aryl group is a fluorescent group. The compounds are useful for the treatment of cancers, especially those with decreased Ras-association domain family 1A (RASSF1A) expression, including prostate cancer. The compounds may reduce DNA methyltransferase activity and/or increase RASSF1A expression. Retention of the compound in a cell is diagnostic for decreased RASSF1A expression, and hence potentially for a cancer cell.
机译:本发明提供咔唑化合物及其前药,其包含与芳基偶联的杂基,其中杂基选自SO 2,S = O,C = O,NH和PO 3。芳基可被一个或多个选自以下的取代基取代:OH,NH 2,NR 1 R 2,NHR 1,OCH 3,OCHR 1 R 2,OCH 2 R 1,OCR 1 R 2 R 3, C = O或S = O,其中R 1,R 2和R 3是烷基,任选地其中与芳基相连的杂基是丹酰基,并且任选地其中与芳基相连的杂基是荧光的组。该化合物可用于治疗癌症,尤其是Ras缔合域家族1A(RASSF1A)表达降低的癌症,包括前列腺癌。所述化合物可降低DNA甲基转移酶活性和/或增加RASSF1A表达。将该化合物保留在细胞中可诊断RASSF1A表达降低,从而可能诊断癌细胞。

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