697273-03-3Relevant academic research and scientific papers
BENZOXAZOLE, BENZTHIAZOLE AND BENZIMIDAZOLE DERIVATIVES USEFUL AS HEPARANASE INHIBITORS
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Page 31, (2010/02/07)
Compounds of formula (I): wherein R1, R2 and R3 are independently, hydrogen, halogen, CF3, OR6, NR7 R8, NR8COR10, NR8SO2R10 or C 1-6 alkyl optionally substituted by hydroxy, C 1-6 alkoxy or NR7R8; R4 is NR8CONR8R9; and R5 formula (Ia) is methods for their
2,3-Dihydro-1,3-dioxo-1H-isoindole-5-carboxylic acid derivatives: A novel class of small molecule heparanase inhibitors
Courtney, Stephen M.,Hay, Philip A.,Buck, Richard T.,Colville, Claire S.,Porter, David W.,Scopes, David I. C.,Pollard, Faye C.,Page, Martin J.,Bennett, James M.,Hircock, Margaret L.,McKenzie, Edward A.,Stubberfield, Colin R.,Turner, Paul R.
, p. 3269 - 3273 (2007/10/03)
A novel class of 2,3-dihydro-1,3-dioxo-1H-isoindole-5-carboxylic acids are described as inhibitors of the endo-β-glucuronidase heparanase. Several of the compounds, for example, 2-[4-propylamino-5-[5-(4-chloro)phenyl-benzoxazol-2- yl]phenyl]-2,3-dihydro-1,3-dioxo-1H-isoindole-5-carboxylic acid (9c), display potent heparanase inhibitory activity (IC50 200-500nM) and have high selectivity (>100-fold) over human β-glucuronidase. They also show anti-angiogenic effects. Such compounds should serve as useful biological tools and may provide a basis for the design of novel therapeutic agents.
