22802-67-1Relevant academic research and scientific papers
Aromatic β-sheet foldamers based on tertiary squaramides
Atcher, Joan,Nagai, Aki,Mayer, Peter,Maurizot, Victor,Tanatani, Aya,Huc, Ivan
, p. 10392 - 10395 (2019)
The preference of N,N-aryl, alkyl tertiary amides for cis conformations has been exploited through the use of tertiary squaramides as hairpin turn units that promote the folding of aromatic β-sheets. Head-to-head aromatic arrangements were shown to prevail in sufficiently long bent aromatic sequences.
EIF4E INHIBITORS AND USES THEREOF
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Paragraph 00506; 00522, (2021/09/11)
The present invention provides compounds inhibiting elF4E activity and compositions and methods of using thereof.
C-H Amination of Arenes with Hydroxylamine
See, Yi Yang,Sanford, Melanie S.
supporting information, p. 2931 - 2934 (2020/04/09)
This Letter describes the development of a TiIII-mediated reaction for the C-H amination of arenes with hydroxylamine. This reaction is applied to a variety of electron-rich (hetero)arene substrates, including a series of natural products and pharmaceuticals. It offers the advantages of mild conditions (room temperature), fast reaction rates (30 min), compatibility with ambient moisture and air, scalability, and the use of inexpensive commercial reagents.
Folding and Assembly of Short α, β, ?-Hybrid Peptides: Minor Variations in Sequence and Drastic Differences in Higher-Level Structures
Zhang, Yukun,Zhong, Yulong,Connor, Alan L.,Miller, Daniel P.,Cao, Ruikai,Shen, Jie,Song, Bo,Baker, Erin S.,Tang, Quan,Pulavarti, Surya V.S.R.K.,Liu, Rui,Wang, Qiwei,Lu, Zhong-Lin,Szyperski, Thomas,Zeng, Huaqiang,Li, Xiaopeng,Smith, Richard D.,Zurek, Eva,Zhu, Jin,Gong, Bing
supporting information, p. 14239 - 14248 (2019/10/11)
Multilevel protein structures typically involve polypeptides of sufficient lengths. Here we report the folding and assembly of seven short tetrapeptides sharing the same types of α-, β-, and aromatic ?-amino acid residues. These are two sets of hybrid peptides, with three members in one set and four in the other, having complementary hydrogen-bonding sequences that were hypothesized to pair into linear H-bonded duplexes. However, instead of undergoing the anticipated pairing, the initially examined three oligomers, 1 and 2a or 2b, differing only in their central αβ hybrid dipeptide sequence, do not associate with each other and exhibit distinctly different folding behavior. Experiments based on NMR and mass spectrometry, along with computational studies and systematic inference, reveal that oligomer 1 folds into an expanded β-turn containing an unusual hybrid α/β-amino acid sequence composed of glycine and β-alanine, two α- A nd β-amino acid residues that are conformationally most flexible, and peptides 2a and 2b adopt a noncanonical, extended helical conformation and dimerize into double helices undergoing rapid conformational exchange or helix inversion. The different central dipeptide sequences, αβ vs βα, result in drastically different intramolecular H-bonding patterns that are responsible for the observed folding behavior of 1 and 2. The revealed turn and double helix have few natural or synthetic counterparts, and provide novel and unique folding prototypes based on which chiral α- A nd β-amino acids are incorporated. The resultant derivatives 1a, 1b, 2c, and 2d follow the same folding and assembling behavior and demonstrate the generality of this system with the formation of expanded β-turns and double helices with enhanced folding stabilities, hampered helix inversion, as well as defined and dominant helical sense. This work has demonstrated the unique capability of synthetic foldamers in generating structures with fascinating folding and assembling behavior. The revealed systems offer ample opportunity for further structural optimization and applications.
FUSED BICYCLIC COMPOUNDS AND USES THEREOF IN MEDICINE
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Paragraph 00196; 00285, (2019/03/05)
Fused bicyclic compounds and uses thereof in medicine. In particular, provided are fused bicyclic compounds used as ASK1 active regulator and and use of the compounds in the manufacture of a drug for treating a disease regulated by ASK1. Further provided are a pharmaceutical composition and a method of treating a disease regulated by ASK1 comprising administering the compounds or pharmaceutical composition thereof.
Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents
An, Baijiao,Wang, Bo,Hu, Jinhui,Xu, Shaoyu,Huang, Ling,Li, Xingshu,Chan, Albert S. C.
, p. 2571 - 2588 (2018/03/26)
Twenty-eight novel selenium-containing 4-anilinoquinazoline derivatives were designed, synthesized, and evaluated as antiproliferative agents. Most of them had significant in vitro activities, particularly for compounds 23a, 25a, and 25d, which also exhibited the most potent antitumor activities against cisplatin-resistant cell lines and the doxorubicin-resistant cell lines, good selectivity toward normal cells, and obvious inhibitory effect on migration of A549 cell lines. Further mechanistic studies revealed that 23a, 25a, and 25d induce G2/M phase arrest and apoptosis in A549 cells, which was associated with a collapse of the mitochondrial membrane potential, alterations in the expression of some cell cycle-related and apoptosis-related proteins, and increasing the intracellular ROS level. Finally, compounds 23a, 25a, and 25d also effectively inhibited the tumor growth in the A549 xenograft model without obvious hints of toxicity. Taken together, these in vitro and in vivo results suggest that 23a, 25a, and 25d may be promising microtubule-stabilizing agents and can be used as a promising lead for the development of new antitumor agents.
3-CARBAMOYLPHENYL-4-CARBOXAMIDE AND ISOPHTALAMIDE DERIVATIVES AS INHIBITORS OF THE WNT SIGNALLING PATHWAY
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Page/Page column 47, (2016/10/17)
The present invention relates to inhibitors of the Wnt signalling pathways of general formula (I) as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative disorder, as a sole agent or in combination with other active ingredients, in which: R1 represents a group selected from: C1-C3-alkoxy-C2-C5-alkyl-, (A), (B), (C), (D), (E), (F), (G) or (H); wherein * indicates the point of attachment to the rest of the molecule; R2 represents a group selected from: (I), (J) or (K); wherein * indicates the point of attachment to the rest of the molecule.
2,4-Pyrimidinediamine Compounds and Their Uses
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, (2015/11/10)
The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
TRIAZOLONE COMPOUNDS AS mPGES-1 INHIBITORS
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, (2014/01/08)
The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.
Electrochemical C-H amination: Synthesis of aromatic primary amines via N -arylpyridinium ions
Morofuji, Tatsuya,Shimizu, Akihiro,Yoshida, Jun-Ichi
supporting information, p. 5000 - 5003 (2013/05/22)
We have developed a new method for C-H amination of aromatic compounds based on electrochemical oxidation of aromatic compounds in the presence of pyridine followed by the reaction of the resulting N-arylpyridinium ions with an alkylamine. This new transformation serves as a powerful method for synthesizing aromatic primary amines from aromatic compounds without using metal catalysts and harsh chemical reagents. High chemoselectivity of the present method is demonstrated by C-H amination of aromatic compounds bearing a nitro group to give a key intermediate for the synthesis of VLA-4 antagonist.
