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.
KATHRYN D. SHEIKH,MIKELL PAIGE,MILTON L. BROWN,PARTHA BANERJEE,SHANKAR JAGADEESH
申请号:
BRPI0917411
公开号:
BRPI0917411A2
申请日:
2009.08.14
申请国别(地区):
BR
年份:
2015
代理人:
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.