149505-94-2Relevant articles and documents
Artificial Macrocycles as Potent p53-MDM2 Inhibitors
Estrada-Ortiz, Natalia,Neochoritis, Constantinos G.,Twarda-Clapa, Aleksandra,Musielak, Bogdan,Holak, Tad A.,D?mling, Alexander
, p. 1025 - 1030 (2017)
Based on a combination of an Ugi four component reaction and a ring closing metathesis, a library of novel artificial macrocyclic inhibitors of the p53-MDM2 interaction was designed and synthesized. These macrocycles, alternatively to stapled peptides, target for the first time the large hydrophobic surface area formed by Tyr67, Gln72, His73, Val93, and Lys94 yielding derivatives with affinity to MDM2 in the nanomolar range. Their binding affinity with MDM2 was evaluated using fluorescence polarization (FP) assay and 1H-15N two-dimensional HSQC nuclear magnetic resonance experiments.
Synthesis of novel 2-pyrrolidinone and pyrrolidine derivatives and study of their inhibitory activity against autotaxin enzyme
Afantitis, Antreas,Aidinis, Vassilis,Gerokonstantis, Dimitrios Triantafyllos,Kokotos, George,Magkrioti, Christiana,Moutevelis-Minakakis, Panagiota,Nikolaou, Aikaterini
, (2020)
Autotaxin (ATX), a glycoprotein (~125 kDa) isolated as an autocrine motility factor from melanoma cells, belongs to a seven-membered family of ectonucleotide pyrophosphatase/phosphodiesterase (ENPP), and exhibits lysophospholipase D activity. ATX is responsible for the hydrolysis of lysophosphatidylcholine (LPC) to produce the bioactive lipid lysophosphatidic acid (LPA), which is upregulated in a variety of pathological inflammatory conditions, including fibrosis, cancer, liver toxicity and thrombosis. Given its role in human disease, the ATX-LPA axis is an interesting target for therapy, and the development of novel potent ATX inhibitors is of great importance. In the present work a novel class of ATX inhibitors, optically active derivatives of 2-pyrrolidinone and pyrrolidine heterocycles were synthesized. Some of them exhibited interesting in vitro activity, namely the hydroxamic acid 16 (IC50 700 nM) and the carboxylic acid 40b (IC50 800 nM), while the boronic acid derivatives 3k (IC50 50 nM), 3l (IC50 120 nM), 3 m (IC50 180 nM) and 21 (IC50 35 nM) were found to be potent inhibitors of ATX.
Diarylcarbonates are a new class of deubiquitinating enzyme inhibitor
Long, Marcus J.C.,Lawson, Ann P.,Baggio, Rick,Qian, Yu,Rozhansky, Lior,Fasci, Domenico,El Oualid, Farid,Weerapana, Eranthie,Hedstrom, Lizbeth
, p. 204 - 211 (2019)
Promiscuous inhibitors of tyrosine protein kinases, proteases and phosphatases are useful reagents for probing regulatory pathways and stabilizing lysates as well as starting points for the design of more selective agents. Ubiquitination regulates many cr
Heptamethine indocyanine dye as well as preparation method and application thereof
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Paragraph 0131; 0146-0148; 0151, (2021/10/05)
The invention provides a heptamethine indocyanine dye as well as a preparation method and an application thereof, and belongs to the technical field of fine chemical engineering. The heptamethine indocyanine dye provided by the invention has a structure a
Rapid and High-Yield Synthesis of [23]Crown Ether: Applied as a Wheel Component in the Formation of Pseudo[2]rotaxane and Synthesis of [2]Catenane with a Dibenzylammonium Dumbbell
Dasgupta, Suvankar,Prakashni, Manisha,Shukla, Rasendra
, p. 7825 - 7831 (2021/06/28)
A facile, rapid, and high yield synthesis of [23]crown ether (X23C7) has been developed from commercially available starting materials, in one step with good to excellent yield. The reaction is completed in 6 h under room temperature conditions, with the highest yield being 81%. The X23C7 macrocycle formed pseudo[2]rotaxane with a dibenzylammonium ion (DBA+) dumbbell, exhibiting strong association (Ka = 2.61 × 103 M-1). Consequently, a [2]catenane was synthesized from a DBA+-based diolefin terminated salt and X23C7 in 81% yield, using a threading-followed-ring-closing-metathesis approach.