111797-22-9Relevant academic research and scientific papers
A new chalcone derivative with promising antiproliferative and anti-invasion activities in glioblastoma cells
Cidade, Honorina,Costa, Bruno M.,Ferreira, Helena,Mendanha, Daniel,Moreira, Joana,Neves, Nuno M.,Pinto, Madalena,Vieira De Castro, Joana
, (2021/06/21)
Glioblastoma (GBM) is the most common and most deadly primary malignant brain tumor. Current therapies are not effective, the average survival of GBM patients after diagnosis being limited to few months. Therefore, the discovery of new treatments for this highly aggressive brain cancer is urgently needed. Chalcones are synthetic and naturally occurring compounds that have been widely investigated as anticancer agents. In this work, three chalcone derivatives were tested regarding their inhibitory activity and selectivity towards GBM cell lines (human and mouse) and a non-cancerous mouse brain cell line. The chalcone 1 showed the most potent and selective cytotoxic effects in the GBM cell lines, being further investigated regarding its ability to reduce critical hallmark features of GBM and to induce apoptosis and cell cycle arrest. This derivative showed to successfully reduce the invasion and proliferation capacity of tumor cells, both key targets for cancer treatment. Moreover, to overcome potential systemic side effects and its poor water solubility, this compound was encapsulated into liposomes. Therapeutic concentrations were incorporated retaining the potent in vitro growth inhibitory effect of the selected compound. In conclusion, our results demonstrated that this new formulation can be a promising starting point for the discovery of new and more effective drug treatments for GBM.
Design, synthesis, biological evaluation of 3,5-diaryl-4,5-dihydro-1H-pyrazole carbaldehydes as non-purine xanthine oxidase inhibitors: Tracing the anticancer mechanism via xanthine oxidase inhibition
Joshi, Gaurav,Sharma, Manisha,Kalra, Sourav,Gavande, Navnath S.,Singh, Sandeep,Kumar, Raj
, (2021/01/19)
Xanthine oxidase (XO) has been primarily targeted for the development of anti-hyperuriciemic /anti-gout agents as it catalyzes the conversion of xanthine and hypoxanthine into uric acid. XO overexpression in various cancer is very well correlated due to r
Design, synthesis, characterization and in silico molecular docking studies and in vivo anti-inflammatory activity of pyrazoline clubbed thiazolinone derivatives
Chawla, Pooja A.,Kulshreshtha, Mayank,Kumar, Yogesh,Shukla, Karuna Shanker,Singh, Deepak Kumar,Ved, Akash
, p. 735 - 748 (2021/10/01)
The pyrazolines give the reactions of aliphatic derivatives, resembling unsaturated compounds in their behavior towards permanganate and nascent hydrogen. This nucleus has been associated with various biological activities, including inflammatory action.
A novel series of benzothiazepine derivatives as tubulin polymerization inhibitors with anti-tumor potency
Wang, Bin,Wang, Li-Ren,Liu, Lu-Lu,Wang, Wei,Man, Ruo-Jun,Zheng, Da-Jun,Deng, Yu-Shan,Yang, Yu-Shun,Xu, Chen,Zhu, Hai-Liang
, (2021/02/02)
In this work, a series of diaryl benzo[b][1,4]thiazepine derivatives D1-D36 were synthesized and screened as tubulin polymerization inhibitors with anti-tumor potency. They were designed by introducing the seven-member ring benzothiazepine as the linker f
A class of novel tubulin polymerization inhibitors exert effective anti-tumor activity via mitotic catastrophe
Zhang, Ya-Liang,Li, Bo-Yan,Yang, Rong,Xia, Lin-Ying,Fan, A-Li,Chu, Yi-Chun,Wang, Lin-Jian,Wang, Zhong-Chang,Jiang, Ai-Qin,Zhu, Hai-Liang
, p. 896 - 910 (2019/01/04)
In current work, a class of novel 4,5-dihydro-1H-pyrazole-1-carboxylate derivatives (E01-E28) were designed, synthesized and evaluated. Among them, the most potent compound E24 exhibited comparable activity against a panel of cancer cells (GI50
Design, synthesis, and carbonic anhydrase inhibition activity of benzenesulfonamide-linked novel pyrazoline derivatives
Abdel-Aziz, Alaa A.-M.,El-Azab, Adel S.,Bua, Silvia,Nocentini, Alessio,Abu El-Enin, Mohamed A.,Alanazi, Mohammed M.,AlSaif, Nawaf A.,Hefnawy, Mohamed M.,Supuran, Claudiu T.
, p. 425 - 431 (2019/03/27)
Carbonic anhydrases (CA, EC 4.2.1.1) are Zinc metalloenzymes and are present throughout most living organisms. Among the catalytically active isoforms are the cytosolic CA I and II, and tumor-associated CA IX and CA XII. The carbonic anhydrase (CA) inhibitory activities of newly synthesized pyrazoline-linked benzenesulfonamides 18–33 against human CA (hCA) isoforms I, II, IX, and XII were measured and compared with that of acetazolamide (AAZ), a standard inhibitor. Potent inhibitory activity against hCA I was exerted by compounds 18–25, with inhibition constant (KI) values of 87.8–244.1 nM, which were greater than that of AAZ (KI, 250.0 nM). Compounds 19, 21, 22, 29, 30, and 32 were proven to have inhibitory activities against hCA IX with KI values (5.5–37.0 nM) that were more effective than or nearly equal to that of AAZ (KI, 25.0 nM). Compounds 20–22, and 30 exerted potent inhibitory activities (KIs, 7.1–10.1 nM) against hCA XII, in comparison with AAZ (KI, 5.7 nM).
Chalcone derivatives targeting mitosis: synthesis, evaluation of antitumor activity and lipophilicity
Pinto, Patricia,Machado, Carmen Mariana,Moreira, Joana,Almeida, José Diogo P.,Silva, Patrícia M.A.,Henriques, Ana C.,Soares, José X.,Salvador, Jorge A.R.,Afonso, Carlos,Pinto, Madalena,Bousbaa, Hassan,Cidade, Honorina
, (2019/10/14)
This study describes the synthesis of a series of chalcones, including pyrazole and α,β-epoxide derivatives, and evaluation of their cell growth inhibitory activity in three human tumor cell lines, as well as their lipophilicity using liposomes as a biomi
Method for preparing 3,4,5-triethoxy-3',4'-dimethoxy chalcone
-
Paragraph 0014; 0015; 0016, (2017/06/14)
The invention provides a method for preparing 3,4,5-triethoxy-3',4'-dimethoxy chalcone. The method comprises the following steps: dissolving 3,4-dimethoxyacetophenone and 3,4,5-triethoxy benzaldehyde in a strong basic ionic liquid, stirring at room temperature, after completing the reaction, leaving to stand a reaction liquid, filtering, washing with water, and drying, thereby obtaining the 3,4,5-triethoxy-3',4'-dimethoxy chalcone. The method is gentle in reaction condition, relatively low in reaction equipment requirement, low in reaction cost and convenient in on-scale production, in addition, environmental pollution caused by organic solvents can be effectively avoided, the yield and the purity of a product prepared with the method are relatively high, and the reaction efficiency can be greatly improved.
Preparation method of 3,4,5-trimethoxy-3',4'-dimethoxy chalcone
-
Paragraph 0014; 0015, (2017/07/20)
The invention provides a preparation method of 3,4,5-trimethoxy-3',4'-dimethoxy chalcone. 3,4-dimethoxyacetophenone and 3,4,5-trimethoxy benzaldehyde are dissolved into strongly basic ionic liquid; room-temperature stirring is performed; after the reaction is completed, still standing is performed on the reaction liquid; filtering, water washing and drying are performed to obtain the 3,4,5-trimethoxy-3',4'-dimethoxy chalcone. The preparation method has the advantages that the reaction conditions are mild; the requirements on the reaction equipment are low; the reaction cost is reduced; the pollution of an organic solvent on the environment is effectively avoided; the large-scale production is convenient; the yield and the purity of the product obtained by the method are high; the reaction efficiency is greatly improved.
Novel polyfunctional pyridines as anticancer and antioxidant agents. Synthesis, biological evaluation and in silico ADME-T Study
Badr, Mona Hany,Rostom, Sherif Ahmed Fawzi,Radwan, Mohammed Fouad
, p. 442 - 454 (2017/05/17)
Two series of novel alkoxylated 2-oxo(imino)-3-pyridinecarbonitriles (structurally-relevant to some reported anticancer pyridines with phosphodiesterase 3A (PDE3A) inhibitory activity) were synthesized and evaluated for their in vitro differential tumor c
