39819-39-1Relevant articles and documents
Rational Design, Synthesis and Evaluation of Oxazolo[4,5-c]-quinolinone Analogs as Novel Interleukin-33 Inhibitors
Byun, Youngjoo,Cho, Haelim,Ho Jeon, Young,Hoon Kim, Kyong,Jang, Geonhee,Kim, Yujin,Lee, Kiho,Lee, Taeyun,Ma, Chao,Paek, Jiwon,Park, Seonghu,Shin -, Yujin,Son, Sang-Hyun,Son, Seyoung,Woo Jung, Yong,Yong Lee, Ki
, p. 3702 - 3712 (2021/11/19)
Interleukin-33 (IL-33) is an epithelial-derived cytokine that plays an important role in immune-mediated diseases such as asthma, atopic dermatitis, and rheumatoid arthritis. Although IL-33 is considered a potential target for the treatment of allergy-rel
NOVEL QUINOLINONE DERIVATIVE AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING ALLERGIC DISEASES SUCH AS ASTHMA OR ATOPIC DERMATITIS INCLUDING THE QUINOLINONE DERIVATIVE AS ACTIVE INGREDIENT
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Paragraph 0028; 0045-0047, (2020/05/29)
The present invention relates to anovel quinolinone derivative compound that regulates intracellular signal transduction mediated by TSLP and IL-33 to exhibit efficacy in preventing or treating allergic diseases such as asthma or atopic dermatitis. The qu
Synthesis and bioactivity of phenyl substituted furan and oxazole carboxylic acid derivatives as potential PDE4 inhibitors
Lin, Yinuo,Ahmed, Wasim,He, Min,Xiang, Xuwen,Tang, Riyuan,Cui, Zi-Ning
, (2020/10/02)
In this present study, a series of 5-phenyl-2-furan and 4-phenyl-2-oxazole derivatives were designed and synthesized as phosphodiesterase type 4 (PDE4) inhibitors. In vitro results showed that the synthesized compounds exhibited considerable inhibitory ac
Discovery of Novel Aryl Carboxamide Derivatives as Hypoxia-Inducible Factor 1α Signaling Inhibitors with Potent Activities of Anticancer Metastasis
Liu, Mingming,Liang, Yuru,Zhu, Zhongzhen,Wang, Jin,Cheng, Xingxing,Cheng, Jiayi,Xu, Binpeng,Li, Rong,Liu, Xinhua,Wang, Yang
supporting information, p. 9299 - 9314 (2019/10/16)
In order to discover novel hypoxia-inducible factor 1 (HIF-1) inhibitors for the cancer metastasis treatment, 68 new aryl carboxamide compounds were synthesized and evaluated for their inhibitory effect by dual luciferase-reporter assay. Based on five rounds of investigation on structure-activity relationships step by step, compound 30m was discovered as the most active inhibitor (IC50 = 0.32 μM) with no obvious cytotoxicity (CC50 > 50 μM). It effectively attenuated hypoxia-induced HIF-1α protein accumulation and reduced transcription of vascular epidermal growth factor in a dose-dependent manner, which was further demonstrated by its inhibitory potency on capillary-like tube formation, angiogenesis of zebrafish as well as cellular migration and invasion. Importantly, compound 30m exhibited antimetastatic potency in breast cancer lung metastasis in the mice model, indicating its promising therapeutic potential for prevention and treatment of tumor metastasis. These results definitely merit attention for further rational design of more efficient HIF-1 inhibitors in the future.
Asymmetric synthesis and biological evaluation of imidazole- and oxazole-containing synthetic lipoxin A4 mimetics (sLXms)
de Gaetano, Monica,Butler, Eibhlín,Gahan, Kevin,Zanetti, Andrea,Marai, Mariam,Chen, Jianmin,Cacace, Antonino,Hams, Emily,Maingot, Catherine,McLoughlin, Alisha,Brennan, Eoin,Leroy, Xavier,Loscher, Christine E.,Fallon, Padraic,Perretti, Mauro,Godson, Catherine,Guiry, Patrick J.
, p. 80 - 108 (2018/11/21)
Lipoxins (LXs) are endogenously generated eicosanoids with potent bio-actions consistent with attenuation of inflammation. The costly synthesis and metabolic instability of LXs may limit their therapeutic potential. Here we report the synthesis and charac
Radical C-H Arylation of Oxazoles with Aryl Iodides: Dppf as an Electron-Transfer Mediator for Cs2CO3
Guo, Zhengwei,Li, Man,Mou, Xue-Qing,He, Gang,Xue, Xiao-Song,Chen, Gong
supporting information, p. 1684 - 1687 (2018/03/23)
A radical C-H arylation reaction of oxazoles with (hetero)aryl iodides using Cs2CO3 as base/electron donor and 1,1′-bis(diphenylphosphino) ferrocene (dppf) as a catalytic SET mediator is reported. The overall reaction likely follows the general base-promoted homolytic aromatic substitution mechanism through a radical-chain pathway. DFT calculations suggest that dppf forms a complex with CsCO3-, enhancing its SET reducing ability to generate an aryl radical from ArI.
Design, synthesis and biological evaluation of 2,4-disubstituted oxazole derivatives as potential PDE4 inhibitors
Li, Ya-Sheng,Hu, De-Kun,Zhao, Dong-Sheng,Liu, Xing-Yu,Jin, Hong-Wei,Song, Gao-Peng,Cui, Zi-Ning,Zhang, Lian-Hui
, p. 1852 - 1859 (2017/03/08)
In this study, a series of pyrazole derivatives containing 4-phenyl-2-oxazole moiety were designed and synthesized in a concise way, some of which exhibited considerable inhibitory activity against PDE4B and blockade of LPS-induced TNF-α release. Compound
Design, synthesis and evaluation of aromatic heterocyclic derivatives as potent antifungal agents
Zhao, Shizhen,Zhang, Xiangqian,Wei, Peng,Su, Xin,Zhao, Liyu,Wu, Mengya,Hao, Chenzhou,Liu, Chunchi,Zhao, Dongmei,Cheng, Maosheng
, p. 96 - 107 (2017/05/31)
To further enhance the anti-Aspergillus efficacy of our previously discovered antifungal lead compounds (1), a series of aromatic heterocyclic derivatives were designed, synthesized and evaluated for in vitro antifungal activity. Many of the target compounds showed good inhibitory activity against Candida albicans and Cryptococcus neoformans. In particular, the isoxazole nuclei were more suited for improving the activity against Aspergillus spp. Among these compounds, 2-F substituted analogues 23g and 23h displayed the most remarkable in vitro activity against Candida spp., C. neoformans, A. fumigatus and fluconazole-resistant C.alb. strains, which is superior or comparable to the activity of the reference drugs fluconazole and voriconazole. Notably, the compounds 23g and 23h exhibited low inhibition profiles for various isoforms of human cytochrome P450 and excellent blood plasma stability.
Synthesis and Molecular Docking Studies of Novel 2-Phenyl-4-Substituted Oxazole Derivatives as Potential Anti-cancer Agents
El-Nezhawy, Ahmed O. H.,Eweas, Ahmad Farouk,Radwan, Mohamed A. A.,El-Naggar, Tarek B. A.
, p. 271 - 279 (2016/02/10)
(Figure presented) A novel series of 2,4-disubstituted oxazole derivatives were synthesized, screened for their anti-tumor activity against three cell lines MCF-7, TK-10, and UACC-62. Molecular docking study was carried out against epidermal growth factor receptor. A new series of 2-phenyl-4-substituted oxazole derivatives were synthesized. A series of chiral α-amino acid derivatives 6, 7, 8, 9, 10, 11, 12, 13, 14, 15 were synthesized by coupling various l-acylated amino acid azide 3. The synthesized compounds were tested for their in vitro antitumor activity against MCF-7, TK-10, and UACC-62 cell lines. Compound 6 exhibited the strongest inhibitory activity against TK cell lines, while compound 12 showed the highest activity against MCF-7 cell lines. Compound 14 was the most active against UACC-62 cell lines. Furthermore, a molecular docking study of the most active compounds was carried out using epidermal growth factor receptor X-ray 3D structure (protein data bank ID 1 M17). Docking results revealed that compound 6 showed the highest binding energy of ΔG = -78.17 Kcal/mol.
Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors
Senger, Johanna,Melesina, Jelena,Marek, Martin,Romier, Christophe,Oehme, Ina,Witt, Olaf,Sippl, Wolfgang,Jung, Manfred
, p. 1545 - 1555 (2016/03/08)
Histone deacetylase 6 (HDAC6) catalyzes the removal of an acetyl group from lysine residues of several non-histone proteins. Here we report the preparation of thiazole-, oxazole-, and oxadiazole-containing biarylhydroxamic acids by a short synthetic proce
