123475-75-2Relevant academic research and scientific papers
Ezrin inhibitors and methods of making and using
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Page/Page column 57; 58, (2017/01/05)
The invention encompasses compound and pharmaceutical composition comprising the compound of the following Formula (I): or pharmaceutically acceptable salts or prodrugs thereof, that are useful for inhibiting ezrin protein in a cell or for inhibiting the growth of a cancer cell.
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.
A SYNTHETIC APPROACH TO DISCORHABDIN ALKALOIDS: HYPERVALENT IODINE OXIDATION OF p-SUBSTITUTED PHENOL DERIVATES TO AZACARBOCYCLIC SPIRODIENONES
Kita, Yasuyuki,Yakura, Takayuki,Tohma, Hirofumi,Kikuchi, Kazumi,Tamura, Yasumitsu
, p. 1119 - 1120 (2007/10/02)
Hypervalent iodine oxidation of O-silylated p-substituted phenols by phenyliodosyl bis(trifluoroacetate) (PIFA) in 2,2,2-trifluoroethanol gave azacarbocyclic spirodienones in good yields.
