872360-18-4Relevant academic research and scientific papers
A METHOD OF USING PROTEASOME INHIBITORS IN COMBINATION WITH HISTONE DEACETYLASE INHIBITORS TO TREAT CANCER
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Page/Page column 105, (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.
TOTAL SYNTHESIS OF SALINOSPORAMIDE A AND ANALOGS THEREOF
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Page/Page column 78, (2008/06/13)
The present invention relates to certain compounds and to methods for the preparation of certain compounds that can be used in the fields of chemistry and medicine. Specifically, described herein are methods for the preparation of various compounds and intermediates, and the compounds and intermediates themselves. More specifically, described herein are methods for synthesizing Salinosporamide A and its analogs from a compound of formula (V).
Stereoselective enzymatic reduction of keto-salinosporamide to (-)-salinosporamide A (NPI-0052)
Manam, Rama Rao,Macherla, Venkat R.,Potts, Barbara C.M.
, p. 2537 - 2540 (2008/02/02)
Salinosporamide A (NPI-0052, 1), a highly potent 20S proteasome inhibitor, has been prepared from its ketone precursor (2) by asymmetric enzymatic reduction. The yields are quantitative with complete stereoselective conversion to the desired product, with no evidence for the undesired diastereomer. This process should lead to new synthetic strategies for the total synthesis of 1.
METHODS OF USING [3.2.0] HETEROCYCLIC COMPOUNDS AND ANALOGS THEREOF FOR THE TREATMENT OF LUNG CANCER
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, (2008/06/13)
Disclosed are methods of treating lung cancer comprising administering to the animal, a therapeutically effective amount of a heterocyclic compound, alone or in combination with another therapeutic.
[3.2.0] Heterocyclic compounds and methods of using the same
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Page/Page column 45, (2008/06/13)
Compounds of Formulae I-VI and derivatives thereof having anti-cancer, anti-inflammatory, and anti-microbial properties and to compositions that include one or more of compounds and their derivatives or analogs having anti-cancer, anti-inflammatory and anti-microbial properties are disclosed. Pharmaceutical compositions comprising such compounds and methods of treating cancer, inflammatory conditions, and microbial infections with the disclosed compounds or the disclosed pharmaceutical compositions are also disclosed.
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
