55370-65-5Relevant articles and documents
Halo-substituted chalcones and azachalcones-inhibited, lipopolysaccharited-stimulated, pro-inflammatory responses through the TLR4-mediated pathway
Shih, Tzenge-Lien,Liu, Ming-Hwa,Li, Chia-Wai,Kuo, Chia-Feng
, (2018/03/21)
A series of B-ring, halo-substituted chalcones and azachalcones were synthesized to evaluate and compare their anti-inflammatory activity. Mouse BALB/c macrophage RAW 264.7 were pre-treated with 10 μg/mL of each compound for one hour before induction of i
Synthesis and cdc25B inhibitory activity evaluation of chalcones
Zhao, Fei,Zhao, Qing-Jie,Zhao, Jing-Xia,Zhang, Da-Zhi,Wu, Qiu-Ye,Jin, Yong-Sheng
, p. 206 - 214 (2013/07/26)
A library of sixty-five chalcones was prepared for screening against the protein phosphatase, cdc25B. From this library, thirteen compounds were found having good inhibitory activity. Two compounds have excellent activity and can be used for the design of
Microwave-assisted synthesis of macrocycles via intramolecular and/or bimolecular Ullmann coupling
Shen, Li,Simmons, Charles J.,Sun, Dianqing
scheme or table, p. 4173 - 4178 (2012/08/28)
Microwave-assisted synthesis of macrocyclic diaryl ethers via intramolecular and/or bimolecular Ullmann coupling is described. Using the optimized conditions, a panel of macrocycles, with different substitution patterns, ring sizes, and linkers, has been successfully synthesized using microwave irradiation. To the best of our knowledge, this work represents the first examples of the microwave-assisted synthesis of macrocyclic diaryl ethers via intramolecular and/or bimolecular Ullmann coupling.
Synthetic chalcones, flavanones, and flavones as antitumoral agents: Biological evaluation and structure-activity relationships
Cabrera, Mauricio,Simoens, Macarena,Falchi, Gabriela,Lavaggi, M. Laura,Piro, Oscar E.,Castellano, Eduardo E.,Vidal, Anabel,Azqueta, Amaia,Monge, Antonio,de Cerain, Adela Lopez,Sagrera, Gabriel,Seoane, Gustavo,Cerecetto, Hugo,Gonzalez, Mercedes
, p. 3356 - 3367 (2008/02/07)
A series of synthetic chalcones, flavanones, and flavones has been synthesized and evaluated for antitumor activity against the human kidney carcinoma cells TK-10, human mammary adenocarcinoma cells MCF-7 (estrogen receptor-positive), and human colon adenocarcinoma cells HT-29. The most active series is the chalcone ones with the best results against TK-10 and HT-29 cells. Fourteen out of 53 analyzed compounds resulted very active against at least two of the studied tumoral cells. Alkaline single cell gel electrophoresis, comet assay, was performed as a study of the chromosomal aberrations promoted by the compounds on normal cells. Four active and two inactive chalcones were studied in the comet assay against normal human kidney cells (HK-2). A structure-activity relationship analysis of these compounds was performed and for 4- and 3,4-disubstituted derivatives a quantitative correlation was obtained in the case of anti-HT-29 activity.
Synthesis and preliminary biological evaluation of 4,6-disubstituted 3-cyanopyridin-2(1H)-ones, a new class of calcium entry blockers
Manna, Fedele,Chimenti, Franco,Bolasco, Adriana,Bizzarri, Bruna,Botta, Maurizio,Tafi, Andrea,Filippelli, Amelia,Rossi, Settimio
, p. 1883 - 1885 (2007/10/03)
The preparation of 3-cyano-4,6-diaryl-pyridin-2(1H)-ones 4a-h, calcium entry blockers related to diltiazem, is described starting from 1,3-diaryl-2-propen-1-ones 5. On preliminary pharmacological tests all compounds are active and some of them show calcium antagonistic activity superior or comparable to diltiazem. (C) 2000 Elsevier Science Ltd. All rights reserved.
Anti-inflammatory, analgesic and antipyretic 4,6-disubstituted 3-cyanopyridine-2-ones and 3-cyano-2-aminopyridines
Manna,Chimenti,Bolasco,Filipelli,Palla,Filippelli,Lampa,Mercantini
, p. 627 - 632 (2007/10/02)
3-Cyano-4-(R,R'-aryl)-6(2-hydroxyphenyl)-2-(1H)pyridones 2a-o and 3-cyano-4-(R-R'-aryl)-6-(2-hydroxyphenyl)-2-aminopyridines were synthesized which showed anti-inflammatory and analgesic activity. Electron withdrawing substituents in 2' or 4' position on