5838-77-7Relevant articles and documents
Preparation of fluorescent polystyrene via ATRP with dimethylamino chalcones as initiator
Zhou, Qiuxuan,Gu, Peiyang,Zhang, Youhao,Li, Najun,Xu, Qingfeng,Zhang, Yong,Lu, Jianmei
, p. 573 - 578 (2014)
4-(3-(4-(Dimethylamino)phenyl)acryloyl)phenyl-2-bromo-2-methylpropanoate (APPBr) was used for the heterogeneous atom transfer radical polymerization (ATRP) of styrene (St) with copper(I) bromide/N,N,N′,N″,N″- pentamethyldiethylenetriamine (PMDETA) catalyt
Chloro and bromo-pyrazole curcumin Knoevenagel condensates augmented anticancer activity against human cervical cancer cells: design, synthesis, in silico docking and in vitro cytotoxicity analysis
Chaudhary, Monika,Kumar, Neeraj,Baldi, Ashish,Chandra, Ramesh,Arockia Babu,Madan, Jitender
, p. 200 - 218 (2019/03/08)
With an endeavor to develop novel curcumin analogs as potential anti-cancer agents, we designed and synthesized a series of Knoevenagel condensates by clubbing pyrazole carbaldehydes at the active methylene carbon atom of the curcumin backbone. Molecular docking studies were carried out to target the proposed derivatives on human kinase β (IKKβ), a potential anti-cancer target. The chloro derivative displayed five hydrogen bond interactions with a docking score of ?11.874 kcal/mol higher than curcumin (docking score = ?7.434 kcal/mol). This was supported by the fact that the propellant shaped derivatives fitted aptly into the binding pocket. Molecular simulations studies were also conducted on the lead molecule and the results figured out that the stable complexes were developed as the minimal deviations per residue of protein within the range of 0.11–0.92 ?. The screened compounds were synthesized, characterized and evaluated in vitro for cytotoxicity against cervical cancer cell line, HeLa using standard cell proliferation assay. Chloro derivative and bromo analog demonstrated IC50 (half maximal inhibitory concentration) value of 14.2 and 18.6 μg/ml, respectively, significantly lower than 42.4 μg/ml of curcumin and higher than 0.008 μg/ml of paclitaxel. Induction of apoptosis was evaluated in the terms of cleavage of caspase-3 enzyme and they also exhibited 69.6 and 65.4% of apoptosis significantly higher than 19.9% induced by curcumin. In conclusion, chloro and bromo derivatives must be evaluated under a set of stringent in vitro and in vivo parameters for translating in to a clinically viable product. Communicated by Ramaswamy H. Sarma.
Synthesis, analgesic and anti-inflammatory activities of chalconyl-incorporated hydrazone derivatives of mefenamic acid
Kumar, Neeraj,Chauhan, Lalit Singh,Sharma, Chandra Shekhar,Dashora, Nipun,Bera, Rajendra
, p. 2580 - 2590 (2015/02/05)
A series of chalconyl-incorporated hydrazone derivatives of mefenamic acid was synthesized in order to obtain new compounds with potential analgesic and anti-inflammatory activity having lesser side effects. The structures of all synthesized compounds were confirmed by means of elemental analysis, IR, 1H NMR, 13C NMR and mass spectra. All compounds were evaluated for their analgesic and anti-inflammatory activities by tail-flick method and carrageenan-induced rat paw edema test, respectively. Among all the synthesized compounds, compounds (4a) and (4j) exhibited the most prominent and consistent anti-inflammatory activity. In acute ulcerogenicity study, it can be concluded that compounds (4a) and (4j) are devoid of the deadlier gastrointestinal toxicities.
Synthesis of chalcones with anticancer activities
Syam, Suvitha,Abdelwahab, Siddig Ibrahim,Al-Mamary, Mohammed Ali,Mohan, Syam
experimental part, p. 6179 - 6195 (2012/09/07)
Several chalcones were synthesized and their in vitro cytotoxicity against various human cell lines, including human breast adenocarcinoma cell line MCF-7, human lung adenocarcinoma cell line A549, human prostate cancer cell line PC3, human adenocarcinoma cell line HT-29 (colorectal cancer) and human normal liver cell line WRL-68 was evaluated. Most of the compounds being active cytotoxic agents, four of them with minimal IC50 values were chosen and studied in detail with MCF-7 cells. The compounds 1, 5, 23, and 25 were capable in eliciting apoptosis in MCF-7 cells as shown by multiparameter cytotoxicity assay and caspase-3/7, -8, and -9 activities (p 0.05). The ROS level showed 1.3-fold increase (p 0.05) at the low concentrations used and thus it was concluded that the compounds increased the ROS level eventually leading to apoptosis in MCF-7 cells through intrinsic as well as extrinsic pathways.
An efficient synthesis of bio-active fluorescent benzylidine tetralones
Kamakshi,Latha, S. Swarna,Reddy
experimental part, p. 944 - 947 (2010/10/18)
Benzylidine tetralones have been synthesized in excellent yields in PEG 600 at room temperature and short time periods. The synthesized compounds are found to have antibacterial activity towards both gram-positive and gram-negative bacteria. The N, N-dialkyl substituted benzylidine tetralones are found to possess fluorescent properties.
Synthesis, antiviral, antituberculostic and antibacterial activities of some novel, 4-(4′-substituted phenyl)-6-(4″-hydroxyphenyl)-2- (substituted imino) pyrimidines
Siddiqui, Anees A.,Rajesh, Ramadoss,Mojahid-Ul-Islam,Alagarsamy, Veerachamy,Meyyanathan, Subramania N.,Kumar, Bommenahalli P.,Suresh, Bhojraj
, p. 17 - 26 (2008/09/18)
A variety of novel 4-[(4′-substituted phenyl)-6-(4″- hydroxyphenyl)-2-substituted imino]pyrimidines were synthesized by reacting 4-(4′-substituted phenyl)-6-(4″-hydroxyphenyl)-2-aminopyrimidines with different substituted aromatic aldehydes, with coumarin
