114645-18-0Relevant academic research and scientific papers
α- and β-Substituted phosphonate analogs of LPA as autotaxin inhibitors
Cui, Peng,McCalmont, William F.,Tomsig, Jose L.,Lynch, Kevin R.,Macdonald, Timothy L.
, p. 2212 - 2225 (2008/09/21)
Autotaxin (ATX) is an attractive pharmacological target due to its lysophospholipase D activity which leads to the production of lysophosphatidic acid (LPA). Blockage of ATX produced LPA by small molecules could be a potential anticancer chemotherapy. In our previous study, we have identified the two β-hydroxy phosphonate analogs of LPA (compounds f17 and f18) as ATX inhibitors. With this work, we investigated α- and β-substituted phosphonate analogs of LPA and evaluated them for ATX inhibitory activity. The stereochemistry of β-hydroxy phosphonates was also studied.
Direct synthesis of N-protected β-amino dimethylhydroxamates: Application to the solid-phase synthesis of a peptide incorporating a new amide bond surrogate ψ[CH2CH2NH]
Limal, David,Quesnel, Anne,Briand, Jean-Paul
, p. 4239 - 4242 (2007/10/03)
A rapid and efficient one-step synthesis of N-protected β-amino dimethylhydroxamates starting from diazo ketones is reported. A Fmoc- protected β-amino aldehyde obtained by reduction of its corresponding dimethylhydroxamate was incorporated during solid p
Aminodiol HIV protease inhibitors. Synthesis and structure - Activity relationships of P1/P1′ compounds: Correlation between lipophilicity and cytotoxicity
Chen, Ping,Cheng, Peter T. W.,Alam, Masud,Beyer, Barbara D.,Bisacchi, Gregory S.,Dejneka, Tamara,Evans, Adelaide J.,Greytok, Jill A.,Hermsmeier, Mark A.,Humphreys, W. Griffith,Jacobs, Glenn A.,Kocy, Octavian,Lin, Pin-Fang,Lis, Karen A.,Marella, Michael A.,Ryono, Denis E.,Sheaffer, Amy K.,Spergel, Steven H.,Sun, Chong-Qing,Tino, Joseph A.,Vite, Gregory,Colonno, Richard J.,Zahler, Robert,Barrish, Joel C.
, p. 1991 - 2007 (2007/10/03)
A series of novel aminodiol inhibitors of HIV protease based on the lead compound 1 with structural modifications at P1′ were synthesized in order to reduce the cytotoxicity of 1. We have observed a high degree of correlation between the lipophilicity and the cytotoxicity of this series of inhibitors. It was found that appropriate substitution at the para position of the P1′ phenyl group of 1 resulted in the identification of equipotent (both against the enzyme and in cell culture) compounds (101, 10m, 10n, and 15c) which possess significantly decreased cytotoxicity.
Retrocarbamate protease inhibitors
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, (2008/06/13)
The invention discloses compounds of the formula STR1 are disclosed as HIV protease inhibitors.
