676498-83-2Relevant academic research and scientific papers
KETONE INHIBITORS OF LYSINE GINGIPAIN
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Paragraph 0377, (2018/04/12)
The present invention provides compounds according to Formula (I) as described herein, and their use for inhibiting the lysine gingipain protease (Kgp) from the bacterium Porphyromonas gingivalis. Also described are gingipain activity probe compounds and methods for assaying gingipain activity are also described, as well as methods for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease.
Design, synthesis and biological evaluation of ezrin inhibitors targeting metastatic osteosarcoma
Paige, Mikell,Kosturko, George,Bulut, Güllay,Miessau, Matthew,Rahim, Said,Toretsky, Jeffrey A.,Brown, Milton L.,üren, Aykut
, p. 478 - 487 (2014/01/17)
Respiratory failure due to pulmonary metastasis is the major cause of death for patients with osteosarcoma. However, the molecular basis for metastasis of osteosarcoma is poorly understood. Recently, ezrin, a member of the ERM family of proteins, has been associated with osteosarcoma metastasis to the lungs. The small molecule NSC 668394 was identified to bind to ezrin, inhibit in vitro and in vivo cell migration, invasion, and metastatic colony survival. Reported herein are the design and synthesis of analogues of NSC 668394, and subsequent functional ezrin inhibition studies. The binding affinity was characterized by surface plasmon resonance technique. Cell migration and invasion activity was determined by electrical cell impedance methodology. Optimization of a series of heterocyclic-dione analogues led to the discovery of compounds 21k and 21m as potential novel antimetastatic agents.
