59263-75-1Relevant academic research and scientific papers
3-ETHYL-3-PHENYLAZEPANE DERIVATIVES HAVING MULTIMODAL ACTIVITY AGAINST PAIN
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Page/Page column 121; 123, (2017/08/07)
The present invention relates to 3-ethyl-3-phenylazepane derivatives having dual pharmacological activity towards both the sigma (σ) receptor and the μ- opioid receptor, to processes of preparation of such compounds, to pharmaceutical compositions compris
Dual protein farnesyltransferase-geranylgeranyltransferase-I inhibitors as potential cancer chemotherapeutic agents
DeSolms, S. Jane,Ciccarone, Terrence M.,MacTough, Suzanne C.,Shaw, Anthony W.,Buser, Carolyn A.,Ellis-Hutchings, Michelle,Fernandes, Christine,Hamilton, Kelly A.,Huber, Hans E.,Kohl, Nancy E.,Lobell, Robert B.,Robinson, Ronald G.,Tsou, Nancy N.,Walsh, Eileen S.,Graham, Samuel L.,Beese, Lorena S.,Taylor, Jeffrey S.
, p. 2973 - 2984 (2007/10/03)
A series of novel diaryl ether lactams have been identified as very potent dual inhibitors of protein farnesyltransferase (FTase) and protein geranylgeranyltransferase I (GGTase-I), enzymes involved in the prenylation of Ras. The structure of the complex formed between one of these compounds and FTase has been determined by X-ray crystallography. These compounds are the first reported to inhibit the prenylation of the important oncogene Ki-Ras4B in vivo. Unfortunately, doses sufficient to achieve this endpoint were rapidly lethal.
Inhibitors of prenyl-protein transferase
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, (2008/06/13)
The present invention is directed to compounds which inhibit prenyl-protein transferase and particularly, the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this in
Inhibitors of prenyl-protein transferase
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, (2008/06/13)
The present invention is directed to azepan-2-one compounds which inhibit prenyl-protein transferase, particularly farnesyl-protein transferase (Ftase), and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
