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Title:
RASSF1A発現およびヒト癌細胞増殖の蛍光調節剤
Document Type and Number:
Japanese Patent JP2012500197
Kind Code:
A
Abstract:
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.

Inventors:
Brown, Milton Elle.
Seek, Catherine Dee.
Paige, Mikel
Bunergy, Pulsa
Jagadishu, shankers
Application Number:
JP2011523005A
Publication Date:
January 05, 2012
Filing Date:
August 14, 2009
Export Citation:
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Assignee:
GEORGETOWN UNIVERSITY
International Classes:
C07D209/88; A61K31/403; A61K45/00; A61P35/00; A61P43/00; C12Q1/02; G01N21/64; G01N33/48; G01N33/68; C12N15/09
Domestic Patent References:
JP2001526276A2001-12-18
JPH0881441A1996-03-26
Foreign References:
WO2007042912A22007-04-19
WO2002049632A12002-06-27
WO2000063171A12000-10-26
Attorney, Agent or Firm:
Hidesaku Yamamoto
Takaaki Yasumura
Natsuki Morishita