872360-17-3Relevant articles and documents
A METHOD OF USING PROTEASOME INHIBITORS IN COMBINATION WITH HISTONE DEACETYLASE INHIBITORS TO TREAT CANCER
-
Page/Page column 103-104, (2008/12/04)
Disclosed are methods of treating cancer comprising administering to the animal, a therapeutically effective amount of proteasome inhibitors and one or more histone deacetylase inhibitor. The animal is a mammal, preferably a human or a rodent.
Enantioselective total synthesis of (-)-salinosporamide A (NPI-0052)
Ling, Taotao,Macherla, Venkat R.,Manam, Rama Rao,McArthur, Katherine A.,Potts, Barbara C. M.
, p. 2289 - 2292 (2008/02/05)
A novel enantioselective total synthesis of 20S proteasome inhibitor Salinosporamide A (NPI-0052; 1) is presented. Key features include intramolecular aldol cyclization of 6 to simultaneously generate the three chiral centers of advanced intermediate 5, cyclohexene ring addition using B-2-cyclohexen-1-yl-9-BBN, and inversion of the C-5 stereocenter by oxidation followed by enantioselective enzymatic reduction.
Structure-activity relationship studies of salinosporamide A (NPI-0052), a novel marine derived proteasome inhibitor
Macherla, Venkat R.,Mitchell, Scott S.,Manam, Rama Rao,Reed, Katherine A.,Chao, Ta-Hsiang,Nicholson, Benjamin,Deyanat-Yazdi, Gordafaried,Mai, Bao,Jensen, Paul R.,Fenical, William F.,Neuteboom, Saskia T. C.,Lam, Kin S.,Palladino, Michael A.,Potts, Barbara C. M.
, p. 3684 - 3687 (2007/10/03)
Salinosporamide A (1, NPI-0052) is a potent proteasome inhibitor in development for treating cancer. In this study, a series of analogues was assayed for cytotoxicity, proteasome inhibition, and inhibition of NF-κB activation. Marked reductions in potency
