17080-23-8Relevant academic research and scientific papers
Chemical Platform for the Preparation of Synthetic Orally Active Peptidomimetics with Hemoregulating Activity
Deigin, Vladislav,Ksenofontova, Olga,Khrushchev, Alexey,Yatskin, Oleg,Goryacheva, Alexandra,Ivanov, Vadim
supporting information, p. 1974 - 1977 (2016/10/22)
A novel chemical platform based on branched piperazine-2,5-dione derivatives (2,5-diketopiperazines) for creating orally available biologically active peptidomimetics has been developed. The platform includes a diketopiperazine scaffold with “built-in” fu
Synthesis and biological evaluation of boron peptide analogues of Belactosin C as proteasome inhibitors
Nakamura, Hiroyuki,Watanabe, Mizuyoshi,Ban, Hyun Seung,Nabeyama, Wataru,Asai, Akira
scheme or table, p. 3220 - 3224 (2010/04/05)
A series of boron peptides 11, 13, 15 and 17 were designed and synthesized as proteasome inhibitors based on the structure of Belactosin C. Matteson homologation was a key step in the synthesis of the boron peptides. Compounds 11a and 13 showed significant inhibition of 20S proteasome chymotrypsin-like (β5) activity (IC50 = 0.28 and 0.51 μM, respectively). Furthermore, like PS-341, compound 11a increased the G2/M cell distribution. A biparametric cytofluorimetric analysis with FITC-labeled annexin V and propidium iodide showed induction of apoptosis by compound 11a at >1 μM concentrations of compound.
MULTIFUNCTIONAL BIOACTIVE COMPOUNDS
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Page/Page column 22, (2008/06/13)
The present invention discloses multifunctional bioactive compounds of formula (I) constituted of an immunoregulatory portion linked to a stabilizer moiety and pharmaceutical compositions thereof useful in the treatment of immune disorders and hemopoietic
