958263-97-3Relevant academic research and scientific papers
10H-BENZO(G)PTERDINE-2,4-DIONE COMPOUNDS FOR THE TREATMENT OF PROLIFERATIVE DISORDERS
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, (2008/12/07)
This invention pertains generally to the field of G-quadruplex ligands, and more particularly, to certain 10H-benzo[g]pteridine-2,4-dione compounds ("BPD compounds"), as described herein, which, inter alia, (selectively) bind (and stabilize) G-quadruplexes. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to (selectively) bind (and stabilize) G-quadruplexes, to inhibit telomerase, to regulate cell proliferation, and in the treatment of proliferative disorders, such as cancer. Formula (I):
Trisubstituted isoalloxazines as a new class of G-quadruplex binding ligands: Small molecule regulation of c-kit oncogene expression
Bejugam, Mallesham,Sewitz, Sven,Shirude, Pravin S.,Rodriguez, Raphael,Shahid, Ramla,Balasubramanian, Shankar
, p. 12926 - 12927 (2008/09/16)
Herein, we report the design, synthesis, biophysical evaluation with primary biological data of 3,8,10-trisubstituted isoalloxazines as a new class of G-quadruplex binding ligands. We have developed a short and robust synthesis for trisubstituted isoalloxazines in good yields. The G-quadruplex binding and stabilization potential of isoalloxazines was assessed by surface plasmon resonance and fluorescence resonance energy transfer assay. The data revealed that these isoalloxazines bind and stabilize G-quadruplex DNA, but not duplex DNA, and exhibit potential for discriminating between DNA quadruplexes. Cell-based experiments using cell lines that express the proto-oncogene c-kit (MCF-7 and HGC-27) showed that such isoalloxazines can inhibit the expression of c-kit. Copyright
